标签归档：glut

GLUT4-IN-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。

GLUT4-IN-2 

GLUT4-IN-2 是一种有效的选择性 GLUT4 抑制剂，对 GLUT1 和 GLUT4 的 IC50s 分别为 11.4 µM 和 6.8 µM。GLUT4-IN-2 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。GLUT4-IN-2 显示出有效的抗肿瘤活性。

GLUT4-IN-2

GLUT4-IN-2 Chemical Structure

CAS No. : 2454113-83-6

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

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生物活性

GLUT4-IN-2 is a potent and selective GLUT4 inhibitor with IC50s of 11.4 µM and 6.8 µM for GLUT1 and GLUT4, respectively. GLUT4-IN-2 induces cell apoptosis and cell cycle arrest at G0/G1phase. GLUT4-IN-2 shows potent antitumor activity[1].

IC50 & Target[1]

GLUT1

11.4 μM (IC50)

GLUT4

6.8 μM (IC50)

体外研究
(In Vitro)

GLUT4-IN-2 (compound F18) induces cell apoptosis and ell cycle arrest at G0/G1phase in CME cells[1].
GLUT4-IN-2 (10 µM; 6 h) decreases the expression of mTOR and CDK2, but increases the expression of GRP78, and cleaved caspase 3 proteins [1].

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

Cell Viability Assay[1]

Cell Line: CME, K562, KCL-22, MB-231, HS-27 cells
Concentration: 1-100 µM
Incubation Time: 48 h
Result: Showed potent cytotoxicity with cytotoxic concentration 50% (CC50) of 1.7, 91.9, 15.3, 45.1, 44.0 µM for CME, K562, KCL-22, MB-231, HS-27 cells, respectively.

Apoptosis Analysis[1]

Cell Line: CEM cells
Concentration: 1.7 µM
Incubation Time: 24 h
Result: Induced cell apoptosis with the percentage of apoptotic cells in the late and early apoptosis region was 55.87% and 1.38%, respectively.

Cell Cycle Analysis[1]

Cell Line: CEM cells
Concentration: 10, 25, 50 µM
Incubation Time: 72 h
Result: Induced cell cycle arrest at G0/G1phase in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: CEM cells
Concentration: 10 µM
Incubation Time: 6 h
Result: Decreased the phosphorylation of mTOR and CDK2 proteins and increased the expression of GRP78, and cleaved caspase 3.

Cell Cytotoxicity Assay[1]

Cell Line: CEM cells
Concentration: 2.5-100 µM
Incubation Time: 48 h
Result: Showed cytotoxicity with the IC50s of 1.7, 187.2 µM for CEM, WBCs cells respectively.

体内研究
(In Vivo)

GLUT4-IN-2 (50 mg/kg; i.p. on day 1–5, 8–12, 15–18) shows antitumor activity in CEM xenograft model[1].

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

Animal Model: 8–10 weeks, SCID mice (CEM xenograft tumor) [1]
Dosage: 50 mg/kg
Administration: I.p.; administered on day 1-5, 8-12, 15-18
Result: Showed potent antitumor activity in vivo.

分子量

385.42

Formula

C17H11N3O4S2
CAS 号

2454113-83-6
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]. Tilekar K,et al. Structure guided design and synthesis of furyl thiazolidinedione derivatives as inhibitors of GLUT 1 and GLUT 4, and evaluation of their anti-leukemic potential. Eur J Med Chem. 2020 Sep 15;202:112603.

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

GLUT inhibitor-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。

GLUT inhibitor-1 

GLUT inhibitor-1 是一种有效且具有口服活性的葡萄糖转运蛋白抑制剂，靶向 GLUT1 和 GLUT3，IC50s 值分别为 242 nM 和 179 nM。GLUT inhibitor-1 具有研究癌症和自身免疫性疾病的潜力。

GLUT inhibitor-1

GLUT inhibitor-1 Chemical Structure

CAS No. : 2421141-40-2

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

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases[1].

IC50 & Target

GLUT1

242 nM (IC50)

GLUT3

179 nM (IC50)

体内研究
(In Vivo)

Summary of the pharmacokinetic parameters of GLUT inhibitor-1 (compound 15b; 30 mg/kg) in mouse and rat[1].

Parameter Mouse Rat
oral Cmax (ng/mL) 2525 1675
oral AUC (ng/mL) 5890 6813
CL (mL/min/kg) 40 37
Vdss (L/Kg) 1.70 4.51
t1/2 (h) 0.785 2.59
F (%) 45.4 49.4
B/Pb 0.05

b: Solubility is determined in PBS buffer solutions.

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

549.67

Formula

C32H35N7O2
CAS 号

2421141-40-2
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]. Liu KG, et al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020;63(10):5201-5211.

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

GLUT inhibitor-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。

GLUT inhibitor-1 

GLUT inhibitor-1 是一种有效且具有口服活性的葡萄糖转运蛋白抑制剂，靶向 GLUT1 和 GLUT3，IC50s 值分别为 242 nM 和 179 nM。GLUT inhibitor-1 具有研究癌症和自身免疫性疾病的潜力。

GLUT inhibitor-1

GLUT inhibitor-1 Chemical Structure

CAS No. : 2421141-40-2

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

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases[1].

IC50 & Target

GLUT1

242 nM (IC50)

GLUT3

179 nM (IC50)

体内研究
(In Vivo)

Summary of the pharmacokinetic parameters of GLUT inhibitor-1 (compound 15b; 30 mg/kg) in mouse and rat[1].

Parameter Mouse Rat
oral Cmax (ng/mL) 2525 1675
oral AUC (ng/mL) 5890 6813
CL (mL/min/kg) 40 37
Vdss (L/Kg) 1.70 4.51
t1/2 (h) 0.785 2.59
F (%) 45.4 49.4
B/Pb 0.05

b: Solubility is determined in PBS buffer solutions.

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

549.67

Formula

C32H35N7O2
CAS 号

2421141-40-2
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]. Liu KG, et al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020;63(10):5201-5211.

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

GLUT inhibitor-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。

GLUT inhibitor-1 

GLUT inhibitor-1 是一种有效且具有口服活性的葡萄糖转运蛋白抑制剂，靶向 GLUT1 和 GLUT3，IC50s 值分别为 242 nM 和 179 nM。GLUT inhibitor-1 具有研究癌症和自身免疫性疾病的潜力。

GLUT inhibitor-1

GLUT inhibitor-1 Chemical Structure

CAS No. : 2421141-40-2

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

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases[1].

IC50 & Target

GLUT1

242 nM (IC50)

GLUT3

179 nM (IC50)

体内研究
(In Vivo)

Summary of the pharmacokinetic parameters of GLUT inhibitor-1 (compound 15b; 30 mg/kg) in mouse and rat[1].

Parameter Mouse Rat
oral Cmax (ng/mL) 2525 1675
oral AUC (ng/mL) 5890 6813
CL (mL/min/kg) 40 37
Vdss (L/Kg) 1.70 4.51
t1/2 (h) 0.785 2.59
F (%) 45.4 49.4
B/Pb 0.05

b: Solubility is determined in PBS buffer solutions.

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.
分子量

549.67

Formula

C32H35N7O2
CAS 号

2421141-40-2
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]. Liu KG, et al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020;63(10):5201-5211.

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