MRS-1191 是一种有效的选择性的 A₃ 腺苷受体 (A₃ adenosine receptor ) 拮抗剂，其 K_B 值为 92 nM，对人 A₃ 受体的 K_i 值为 31.4 nM，对 CHO 细胞的 IC₅₀ 值为 120 nM。

MRS-1191 is a potent and selective A 3 adenosine receptor antagonist with a K B value of 92 nM, a K i value of 31.4 nM for human A 3 receptor and an IC 50 of 120 nM for CHO cells.

Solid

Ki: 31.4 nM (human A3 adenosine receptor)

The effects of putative A3 adenosine receptor antagonist of MRS-1191 is characterized in receptor binding and functional assays. MRS-1191 is found to be competitive in saturation binding studies using the agonist radioligand [I]AB-MECA (N-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide) at cloned human brain A3 receptor expressed in HEK-293 cells. Antagonism is demonstrated in functional assays consisting of agonist-induced inhibition of adenylate cyclase and the stimulation of binding of [S]guanosine 5-O-(3-thiotriphosphate) ([S]GTP-gamma-S) to the associated G-proteins. MRS-1191 with a KB value of 92 nM, proves to be highly selective for human A3 receptor vs human A1 receptor-mediated effects on adenylate cyclase. has not independently confirmed the accuracy o

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Jacobson KA, et al. Pharmacological characterization of novel A3 adenosine receptor-selective antagonists. Neuropharmacology. 1997 Sep;36(9):1157-65.

In Vitro: DMSO : 250 mg/mL (523.51 mM; Need ultrasonic)配制储备液