A2A receptor antagonist 2 | whatman (沃特曼)

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A2A receptor antagonist 2

A2A receptor antagonist 2 (Compound 57) 是一个有效的、高选择性的 adenosine A_2A receptor 拮抗剂， IC₅₀ 值为8.3 nM。

A2A receptor antagonist 2 Chemical Structure

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生物活性

A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A_2A receptor (A_2AR) 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 A_2AR 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)
C_max (ng/mL)	1091 ± 129^a	106 ± 33.0	41.8 ± 2.75
AUC_0-last (ng/mL*h)	767 ± 107	145 ± 25.9	812 ± 12.0
AUC_0-t (ng/mL*h)	764 ± 107	139 ± 25.9	444 ± 13.3
T_1/2 (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.

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