标签归档：antagonist

Estrogen receptor antagonist 1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Estrogen receptor antagonist 1 

Estrogen receptor antagonist 1 是一种选择性的 estrogen receptor 拮抗剂。雌激素 (E2) 和雌激素α受体 (ERα) 是乳腺癌发展的重要驱动因素。Estrogen receptor antagonist 1 具有研究乳腺癌疾病的潜力 (摘自专利 WO2021249533A1，化合物 4)。

Estrogen receptor antagonist 1

Estrogen receptor antagonist 1 Chemical Structure

CAS No. : 2751609-45-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4)[1].

分子量

515.59

Formula

C28H33F4N5
CAS 号

2751609-45-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang Yan, et al. Estrogen receptor modulator compounds and their uses. Patent WO2021249533A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Estrogen receptor antagonist 1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Estrogen receptor antagonist 1 

Estrogen receptor antagonist 1 是一种选择性的 estrogen receptor 拮抗剂。雌激素 (E2) 和雌激素α受体 (ERα) 是乳腺癌发展的重要驱动因素。Estrogen receptor antagonist 1 具有研究乳腺癌疾病的潜力 (摘自专利 WO2021249533A1，化合物 4)。

Estrogen receptor antagonist 1

Estrogen receptor antagonist 1 Chemical Structure

CAS No. : 2751609-45-5

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Estrogen receptor antagonist 1 is a selective estrogen receptor antagonist. Estrogen (E2) and estrogen alpha receptor (ERα) are important drivers of breast cancer development. Estrogen receptor antagonist 1 has the potential for the research of breast cancer diseases (extracted from patent WO2021249533A1, compound 4)[1].

分子量

515.59

Formula

C28H33F4N5
CAS 号

2751609-45-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Zhang Yan, et al. Estrogen receptor modulator compounds and their uses. Patent WO2021249533A1.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

XIAP/cIAP1 antagonist-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

XIAP/cIAP1 antagonist-1 

XIAP/cIAP1 antagonist-1 是一种有效的且具有口服活性的 XIAP/cIAP1 拮抗剂，XIAP 和 cIAP1 的 EC50 值分别为 5.1 nM 和 0.32 nM。XIAP/cIAP1 antagonist-1 在体内以剂量依赖方式抑制肿瘤生长。

XIAP/cIAP1 antagonist-1

XIAP/cIAP1 antagonist-1 Chemical Structure

CAS No. : 1403898-55-4

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo[1].

IC50 & Target[1]

XIAP

5.1 nM (IC50)

cIAP1

0.32 nM (IC50)

体外研究
(In Vitro)

XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

XIAP/cIAP1 antagonist-1 (compound 26) (7.5, 15, 30 mg/kg; p.o.; daily for 24 days) inhibits the tumor growth in dose-dependent manner[1].
XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg[1].
Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice[1].

dose (mg/kg) route Tmax (h) Cmax (µg/mL) CLp (mL/min/kg) Vss (L/kg) half life (h) AUC (µg·h/mL) F (%)
1 IV 40.9 6.4 3.0 0.41
5 PO 2 0.12 1.8 0.45 22
30 PO 1 1.7 12.1

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; daily for 24 days
Result: Inhibited the tumor growth in dose-dependent manner.
Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage:
Administration: 1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
Result: Showed oral bioavailability (F=22%).

分子量

509.66

Formula

C29H40FN5O2
CAS 号

1403898-55-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tamanini E, et al. Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP). J Med Chem. 2017; 60(11):4611-4625.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

XIAP/cIAP1 antagonist-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

XIAP/cIAP1 antagonist-1 

XIAP/cIAP1 antagonist-1 是一种有效的且具有口服活性的 XIAP/cIAP1 拮抗剂，XIAP 和 cIAP1 的 EC50 值分别为 5.1 nM 和 0.32 nM。XIAP/cIAP1 antagonist-1 在体内以剂量依赖方式抑制肿瘤生长。

XIAP/cIAP1 antagonist-1

XIAP/cIAP1 antagonist-1 Chemical Structure

CAS No. : 1403898-55-4

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo[1].

IC50 & Target[1]

XIAP

5.1 nM (IC50)

cIAP1

0.32 nM (IC50)

体外研究
(In Vitro)

XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

XIAP/cIAP1 antagonist-1 (compound 26) (7.5, 15, 30 mg/kg; p.o.; daily for 24 days) inhibits the tumor growth in dose-dependent manner[1].
XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg[1].
Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice[1].

dose (mg/kg) route Tmax (h) Cmax (µg/mL) CLp (mL/min/kg) Vss (L/kg) half life (h) AUC (µg·h/mL) F (%)
1 IV 40.9 6.4 3.0 0.41
5 PO 2 0.12 1.8 0.45 22
30 PO 1 1.7 12.1

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; daily for 24 days
Result: Inhibited the tumor growth in dose-dependent manner.
Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage:
Administration: 1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
Result: Showed oral bioavailability (F=22%).

分子量

509.66

Formula

C29H40FN5O2
CAS 号

1403898-55-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tamanini E, et al. Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP). J Med Chem. 2017; 60(11):4611-4625.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

XIAP/cIAP1 antagonist-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

XIAP/cIAP1 antagonist-1 

XIAP/cIAP1 antagonist-1 是一种有效的且具有口服活性的 XIAP/cIAP1 拮抗剂，XIAP 和 cIAP1 的 EC50 值分别为 5.1 nM 和 0.32 nM。XIAP/cIAP1 antagonist-1 在体内以剂量依赖方式抑制肿瘤生长。

XIAP/cIAP1 antagonist-1

XIAP/cIAP1 antagonist-1 Chemical Structure

CAS No. : 1403898-55-4

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

XIAP/cIAP1 antagonist-1 is a potent and orally active XIAP/cIAP1 antagonist with EC50s of 5.1 nM and 0.32 nM for XIAP and cIAP1, respectively. XIAP/cIAP1 antagonist-1 inhibits the tumor growth in dose-dependent manner in vivo[1].

IC50 & Target[1]

XIAP

5.1 nM (IC50)

cIAP1

0.32 nM (IC50)

体外研究
(In Vitro)

XIAP/cIAP1 antagonist-1 (compound 26) shows antiproliferation activity in MDA-MB-231 cells witn an IC50 value of 4.4 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

XIAP/cIAP1 antagonist-1 (compound 26) (7.5, 15, 30 mg/kg; p.o.; daily for 24 days) inhibits the tumor growth in dose-dependent manner[1].
XIAP/cIAP1 antagonist-1 (1 mg/kg for i.v.; 5, 30 mg/kg for p.o.) shows oral bioavailability (F=22%) at 5 mg/kg[1].
Pharmacokinetic Parameters of XIAP/cIAP1 antagonist-1 in Balb/c SCID mice[1].

dose (mg/kg) route Tmax (h) Cmax (µg/mL) CLp (mL/min/kg) Vss (L/kg) half life (h) AUC (µg·h/mL) F (%)
1 IV 40.9 6.4 3.0 0.41
5 PO 2 0.12 1.8 0.45 22
30 PO 1 1.7 12.1

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: PO; daily for 24 days
Result: Inhibited the tumor growth in dose-dependent manner.
Animal Model: Balb/c SCID mice bearing MDA-MB-231 xenografts[1]
Dosage:
Administration: 1 mg/kg for i.v.; 5, 30 mg/kg for p.o.
Result: Showed oral bioavailability (F=22%).

分子量

509.66

Formula

C29H40FN5O2
CAS 号

1403898-55-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Tamanini E, et al. Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP). J Med Chem. 2017; 60(11):4611-4625.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 7

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 7 

CXCR2 antagonist 7 (compound 19) 是一种有效的 CXCR2 拮抗剂。CXCR2 antagonist 7 显示出有效的 CXCR2 结合亲和力 (IC50=0.044 µM) 和钙动员 (IC50=0.66 µM)。

CXCR2 antagonist 7

CXCR2 antagonist 7 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].

IC50 & Target

CXCR2

0.044 μM (IC50)

分子量

352.36

Formula

C14H14F2N6OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 7

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 7 

CXCR2 antagonist 7 (compound 19) 是一种有效的 CXCR2 拮抗剂。CXCR2 antagonist 7 显示出有效的 CXCR2 结合亲和力 (IC50=0.044 µM) 和钙动员 (IC50=0.66 µM)。

CXCR2 antagonist 7

CXCR2 antagonist 7 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].

IC50 & Target

CXCR2

0.044 μM (IC50)

分子量

352.36

Formula

C14H14F2N6OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 7

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 7 

CXCR2 antagonist 7 (compound 19) 是一种有效的 CXCR2 拮抗剂。CXCR2 antagonist 7 显示出有效的 CXCR2 结合亲和力 (IC50=0.044 µM) 和钙动员 (IC50=0.66 µM)。

CXCR2 antagonist 7

CXCR2 antagonist 7 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 7 (compound 19) is a potent CXCR2 antagonist. CXCR2 antagonist 7 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].

IC50 & Target

CXCR2

0.044 μM (IC50)

分子量

352.36

Formula

C14H14F2N6OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 6 

CXCR2 antagonist 6 (compound 35c) 是一种有效的 CXCR2 拮抗剂。CXCR2 antagonist 6 显示出有效的 CXCR2 结合亲和力 (IC50=0.43 µM) 和钙动员 (IC50=0.11 µM)。

CXCR2 antagonist 6

CXCR2 antagonist 6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].

IC50 & Target

CXCR2

0.43 μM (IC50)

分子量

362.40

Formula

C17H16F2N4OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 5 

CXCR2 antagonist 5 (compound 25) 是一种有效的 CXCR2 拮抗剂。 CXCR2 antagonist 5 显示出有效的 CXCR2 结合亲和力 (IC50=0.013 µM) 和钙动员 (IC50=0.1 µM)。

CXCR2 antagonist 5

CXCR2 antagonist 5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM)[ 1].

IC50 & Target

CXCR2

0.013 μM (IC50)

分子量

352.36

Formula

C15H14F2N4O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 6 

CXCR2 antagonist 6 (compound 35c) 是一种有效的 CXCR2 拮抗剂。CXCR2 antagonist 6 显示出有效的 CXCR2 结合亲和力 (IC50=0.43 µM) 和钙动员 (IC50=0.11 µM)。

CXCR2 antagonist 6

CXCR2 antagonist 6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].

IC50 & Target

CXCR2

0.43 μM (IC50)

分子量

362.40

Formula

C17H16F2N4OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 6

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 6 

CXCR2 antagonist 6 (compound 35c) 是一种有效的 CXCR2 拮抗剂。CXCR2 antagonist 6 显示出有效的 CXCR2 结合亲和力 (IC50=0.43 µM) 和钙动员 (IC50=0.11 µM)。

CXCR2 antagonist 6

CXCR2 antagonist 6 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 6 (compound 35c) is a potent CXCR2 antagonist. CXCR2 antagonist 6 shows potent CXCR2 binding affinity (IC50=0.044 µM) and calcium mobilization (IC50=0.66 µM)[ 1].

IC50 & Target

CXCR2

0.43 μM (IC50)

分子量

362.40

Formula

C17H16F2N4OS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 5 

CXCR2 antagonist 5 (compound 25) 是一种有效的 CXCR2 拮抗剂。 CXCR2 antagonist 5 显示出有效的 CXCR2 结合亲和力 (IC50=0.013 µM) 和钙动员 (IC50=0.1 µM)。

CXCR2 antagonist 5

CXCR2 antagonist 5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM)[ 1].

IC50 & Target

CXCR2

0.013 μM (IC50)

分子量

352.36

Formula

C15H14F2N4O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

CXCR2 antagonist 5

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CXCR2 antagonist 5 

CXCR2 antagonist 5 (compound 25) 是一种有效的 CXCR2 拮抗剂。 CXCR2 antagonist 5 显示出有效的 CXCR2 结合亲和力 (IC50=0.013 µM) 和钙动员 (IC50=0.1 µM)。

CXCR2 antagonist 5

CXCR2 antagonist 5 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

CXCR2 antagonist 5 (compound 25) is a potent CXCR2 antagonist. CXCR2 antagonist 5 shows potent CXCR2 binding affinity (IC50=0.013 µM) and calcium mobilization (IC50=0.1 µM)[ 1].

IC50 & Target

CXCR2

0.013 μM (IC50)

分子量

352.36

Formula

C15H14F2N4O2S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Van Hoof M, et al. Identification of novel chemotypes as CXCR2 antagonists via a scaffold hopping approach from a thiazolo[4,5-d]pyrimidine. Eur J Med Chem. 2022; 235:114268.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

A2A receptor antagonist 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

A2A receptor antagonist 2 

A2A receptor antagonist 2 (Compound 57) 是一个有效的、高选择性的 adenosine A2A receptor 拮抗剂， IC50 值为8.3 nM。

A2A receptor antagonist 2

A2A receptor antagonist 2 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM[1].

IC50 & Target

A2AR

8.3 nM (IC50)

体外研究
(In Vitro)

A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A2AR agonist) [1].
A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 10 μM
Incubation Time: Overnight
Result: Increased IL-2 production in the presence of NECA

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 and Jurkat T cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Completely reversed NECA’s suppression of the cytotoxic function of Jurkat T cells.

体内研究
(In Vivo)

A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1]
Dosage: 2 or 10 mg/kg
Administration: Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)
Result: PK profiles of A2A receptor antagonist 2 (n = 3)[1]

Parameters
Dosing Route IV (2 mg/kg) PO (10 mg/kg) IP (10mg/kg)
Cmax (ng/mL) 1091 ± 129a 106 ± 33.0 41.8 ± 2.75
AUC0-last (ng/mL*h) 767 ± 107 145 ± 25.9 812 ± 12.0
AUC0-t (ng/mL*h) 764 ± 107 139 ± 25.9 444 ± 13.3
T1/2 (h) 2.05 ± 0.94 2.55 ± 2.39 17.6 ± 0.68
F (%) / 3.78% 11.6%

a This value means C0 = 1091 ± 129 ng/mL

分子量

493.53

Formula

C25H28FN7O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Fazhi Yu, et al. Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8H)-one Derivatives as Novel Potent Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2022 Mar 10;65(5):4367-4386.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

A2A receptor antagonist 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

A2A receptor antagonist 2 

A2A receptor antagonist 2 (Compound 57) 是一个有效的、高选择性的 adenosine A2A receptor 拮抗剂， IC50 值为8.3 nM。

A2A receptor antagonist 2

A2A receptor antagonist 2 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM[1].

IC50 & Target

A2AR

8.3 nM (IC50)

体外研究
(In Vitro)

A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A2AR agonist) [1].
A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 10 μM
Incubation Time: Overnight
Result: Increased IL-2 production in the presence of NECA

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 and Jurkat T cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Completely reversed NECA’s suppression of the cytotoxic function of Jurkat T cells.

体内研究
(In Vivo)

A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1]
Dosage: 2 or 10 mg/kg
Administration: Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)
Result: PK profiles of A2A receptor antagonist 2 (n = 3)[1]

Parameters
Dosing Route IV (2 mg/kg) PO (10 mg/kg) IP (10mg/kg)
Cmax (ng/mL) 1091 ± 129a 106 ± 33.0 41.8 ± 2.75
AUC0-last (ng/mL*h) 767 ± 107 145 ± 25.9 812 ± 12.0
AUC0-t (ng/mL*h) 764 ± 107 139 ± 25.9 444 ± 13.3
T1/2 (h) 2.05 ± 0.94 2.55 ± 2.39 17.6 ± 0.68
F (%) / 3.78% 11.6%

a This value means C0 = 1091 ± 129 ng/mL

分子量

493.53

Formula

C25H28FN7O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Fazhi Yu, et al. Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8H)-one Derivatives as Novel Potent Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2022 Mar 10;65(5):4367-4386.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

A2A receptor antagonist 2

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

A2A receptor antagonist 2 

A2A receptor antagonist 2 (Compound 57) 是一个有效的、高选择性的 adenosine A2A receptor 拮抗剂， IC50 值为8.3 nM。

A2A receptor antagonist 2

A2A receptor antagonist 2 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM[1].

IC50 & Target

A2AR

8.3 nM (IC50)

体外研究
(In Vitro)

A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A2AR agonist) [1].
A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Jurkat T cells
Concentration: 10 μM
Incubation Time: Overnight
Result: Increased IL-2 production in the presence of NECA

Cell Cytotoxicity Assay[1]

Cell Line: HCT116 and Jurkat T cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Completely reversed NECA’s suppression of the cytotoxic function of Jurkat T cells.

体内研究
(In Vivo)

A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1]
Dosage: 2 or 10 mg/kg
Administration: Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)
Result: PK profiles of A2A receptor antagonist 2 (n = 3)[1]

Parameters
Dosing Route IV (2 mg/kg) PO (10 mg/kg) IP (10mg/kg)
Cmax (ng/mL) 1091 ± 129a 106 ± 33.0 41.8 ± 2.75
AUC0-last (ng/mL*h) 767 ± 107 145 ± 25.9 812 ± 12.0
AUC0-t (ng/mL*h) 764 ± 107 139 ± 25.9 444 ± 13.3
T1/2 (h) 2.05 ± 0.94 2.55 ± 2.39 17.6 ± 0.68
F (%) / 3.78% 11.6%

a This value means C0 = 1091 ± 129 ng/mL

分子量

493.53

Formula

C25H28FN7O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Fazhi Yu, et al. Design, Synthesis, and Bioevaluation of 2-Aminopteridin-7(8H)-one Derivatives as Novel Potent Adenosine A2A Receptor Antagonists for Cancer Immunotherapy. J Med Chem. 2022 Mar 10;65(5):4367-4386.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

NOD1/2 antagonist-1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NOD1/2 antagonist-1 

NOD1/2 antagonist-1 (compound 36b) 是一种有效的 NOD1/2 双拮抗剂，其IC50 值分别为 1.13 (NOD1) 和 0.77 μM (NOD2)。NOD1/2 antagonist-1 有可接受的 T1/2 (67.6 min)。NOD1/2 antagonist-1 (compound 36b) 可提高紫杉醇 (PTX) 的抗肿瘤作用。

NOD1/2 antagonist-1

NOD1/2 antagonist-1 Chemical Structure

CAS No. : 2704623-69-6

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

NOD1/2 antagonist-1 (compound 36b) is a potent NOD1/2 (nucleotide-binding oligomerization domain-like receptor 1/2) dual antagonist, with IC50 values of 1.13 (NOD1) and 0.77 μM (NOD2), respectively. NOD1/2 antagonist-1 has a acceptable T1/2 (67.6 min). NOD1/2 antagonist-1 (compound 36b) can improve the antitumor efficacy of Paclitaxel (PTX)[1].

IC50 & Target

NOD1

1.13 μM (IC50)

NOD2

0.77 μM (IC50)

体外研究
(In Vitro)

NOD1/2 antagonist-1 (compound 36b) (0-10 μM, 3 h) inhibits C12-iE-DAP-induced or MDP-induced NF-κB activation[1].
NOD1/2 antagonist-1 (0-10 μM, 1 h) suppresses inflammation via NOD1 and NOD2 activation[1].
NOD1/2 antagonist-1 (0-10 μM, 1 h) consistently and dose-dependently reduces the transcription of IL-6, TNF-α and IL-8, respectively[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line: HEK-Blue hNOD1 and HEK-Blue hNOD2 cells[1]
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 3 h
Result: Inhibited C12-iE-DAP-induced or MDP-induced NF-κB activation, and had no or little effect on cell growth.

Western Blot Analysis

Cell Line: THP-1 cells[1]
Concentration: 1, 10 μM
Incubation Time: 1 h
Result: Prevented the increases in p-RIP2, p-IKKα/β, p-p65, p-p38, and p-JNK and the degradation of IκBα in a dose-dependent manner, and blocked NOD1-and NOD2-mediated inflammatory cytokine secretion in THP-1 cells.

RT-PCR

Cell Line: THP-1 cells[1]
Concentration: 1, 10 μM
Incubation Time: 1 h
Result: Consistently and dose-dependently reduced the transcription of IL-6, TNF-α and IL-8 stimulated by C12-iE-DAP or MDP, respectively.

体内研究
(In Vivo)

NOD1/2 antagonist-1 (compound 36b) (50 mg/kg, IV, once every other day, for 16 days) improves the antitumor efficacy of PTX in B16 tumor-bearing model[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (6-8 weeks old, male, B16 tumor-bearing model, 4 groups, n = 7 each group)[1]
Dosage: 50 mg/kg (36b), 50 mg/kg (36b) + 12 mg/kg (PTX) (formulated in DMSO/Cremophor EL/saline at 5:5:90(v:v:v))
Administration: IV, once every other day (36b), once every 4 days (PTX), for 16 days
Result: Significantly reduced tumor growth compared with PTX treatment alone, and the tumor weight inhibitory rate increased from 64.07% to 85.46%.

分子量

663.03

Formula

C32H28ClF5N4O4
CAS 号

2704623-69-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Ma Y, Yang J, Wei X, et al. Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy. Eur J Med Chem. 2020;207:112723.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

RXR antagonist 1

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RXR antagonist 1 

RXR antagonist 1 (compound 6a) 是一种类视黄醇 X 受体 (Retinoid X Receptor (RXR)) 调节剂。RXR antagonist 1 具有较强的 RXR 拮抗活性，其 pA2 为 8.06。RXR antagonist 1 可用于 2 型糖尿病的研究。

RXR antagonist 1

RXR antagonist 1 Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

RXR antagonist 1 (compound 6a) is a retinoid X receptor (RXR) modulator. RXR antagonist 1 shows potent RXR-antagonistic activity, with a pA2 of 8.06. RXR antagonist 1 can be used for type 2 diabetes research[1].

IC50 & Target

RXR

8.06 (pA2)

体外研究
(In Vitro)

RXR antagonist 1 (compound 6a) shows potent RXR-antagonistic activities at 1 μM[1].
RXR antagonist 1 shows competitive binding to the LBP in hRXRα-LBD, with Ki of 0.384 ± 0.072, Kd of 0.277 ± 0.038, and Ki/Kd of 1.39[1].
The cell permeability of RXR antagonist 1 shows no correlation with RXR-antagonistic activity[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

502.57

Formula

C28H33F3N2O3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Masaki Watanabe, et al. Increased Molecular Flexibility Widens the Gap between Ki and Kd values in Screening for Retinoid X Receptor Modulators. ACS Med. Chem. Lett. 2022, 13, 2, 211-217.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

多肽定制VIP Antagonist|Vasoactive Intestinal Peptide Antagonist 编码 [125093-93-8]

发表于由

上海金畔生物科技有限公司可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称 VIP Antagonist|Vasoactive Intestinal Peptide Antagonist
编码 [125093-93-8]
别名 VIP Antagonist|Vasoactive Intestinal Peptide Antagonist
纯度 80%，90%，95%，98%，99%
重量 1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写） KPRRPYTDNYTRLRKQMAVKKYLNSILN-NH2
序列（三字母缩写） Lys-Pro-Arg-Arg-Pro-Tyr-Thr-Asp-Asn-Tyr-Thr-Arg-Leu-Arg-Lys-Gln-Met-Ala-Val-Lys-Lys-Tyr-Leu-Asn-Ser-Ile-Leu-Asn-NH2
基本描述
溶解度
分子量 3467.13
化学式 C154H257N49O40S
存储条件 Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents VIP Antagonist|Vasoactive Intestinal Peptide Antagonist 编码 [125093-93-8]
Figures VIP Antagonist|Vasoactive Intestinal Peptide Antagonist 编码 [125093-93-8]
Reference
C端
N端
化学桥