MRS2279 diammonium 

MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a K_i value of 2.5 nM and an IC₅₀ value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pK_b value of 8.05^[1][2][3].

MRS2279 diammonium 能拮抗火鸡红细胞膜中 2-MeSADP 刺激的磷酸肌醇形成，pK_b 值为 7.75^[2]。
MRS2279 diammonium 具有高亲和力竞争性拮抗作用，在 1321N1 人星形细胞瘤细胞中的 pK_b值为 8.10^[2]。
MRS2279 diammonium 对 P2Y1 受体具有特异性拮抗作用，但显示其同源激动剂对人类 P2Y2、P2Y4、P2Y6 或 P2Y11 受体的激活没有影响^[2]。
MRS2279 diammonium 显示没有能力阻断 ADP 通过Gi/腺苷酸环化酶连接血小板 P2Y 受体抑制环 AMP 积累^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

MRS2279 diammonium (2 μL，1 nM；脑室内注射；机械通气前 30 分钟给药) 能减少高压通气小鼠因机械通气引起的小鼠脑损伤^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

503.77

C₁₃H₂₄ClN₇O₈P₂

2387505-47-5

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Nandanan E, et al. Synthesis, biological activity, and molecular modeling of ribose-modified deoxyadenosine bisphosphate analogues as P2Y(1) receptor ligands. J Med Chem. 2000;43(5):829-842.  [Content Brief]

  [2]. Boyer JL, et al, Ravi RG, Jacobson KA, Harden TK. 2-Chloro N(6)-methyl-(N)-methanocarba-2'-deoxyadenosine-3',5'-bisphosphate is a selective high affinity P2Y(1) receptor antagonist. Br J Pharmacol. 2002;135(8):2004-2010.  [Content Brief]

  [3]. Wei W, et al. Mechanical ventilation induces lung and brain injury through ATP production, P2Y1 receptor activation and dopamine release. Bioengineered. 2022 Feb;13(2):2346-2359.  [Content Brief]