MRS2179 tetrasodium hydrate_product_DataBase

Bioactivity	MRS2179 tetrasodium hydrate is a competitive P2Y1 receptor antagonist, with a Kb of 102 nM and a pA2 of 6.99 for turkey P2Y1 receptor. MRS2179 tetrasodium hydrate is selective for P2Y1 over P2X1 (IC50=1.15 µM), P2X3 (12.9 µM), P2X2, P2X4, P2Y2, P2Y4, and P2Y6 receptors[1][2]. MRS2179 tetrasodium hydrate inhibits platelet aggregation[3].
In Vivo	MRS2179 tetrasodium hydrate (50 mg/kg; i.p.) prolongs the bleeding time[3]. Animal Model:
Name	MRS2179 tetrasodium hydrate
Formula	C11H13N5O9P2Na4.3?H2O
Molar Mass	576.21
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[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. [2]. von Kügelgen I. Pharmacological profiles of cloned mammalian P2Y-receptor subtypes. Pharmacol Ther. 2006;110(3):415-432. [3]. Baurand A, Raboisson P, Freund M, et al. Inhibition of platelet function by administration of MRS2179, a P2Y1 receptor antagonist. Eur J Pharmacol. 2001;412(3):213-221.

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