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MRS2179(ammonium salt hydrate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRS2179(ammonium salt hydrate)图片
规格:98%
分子量:425.2
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
A P2Y1 receptor antagonist
货号:ajcx24242
CAS:N/A
分子式:C11H17N5O9P2•XNH3 [XH2O]
分子量:425.2
溶解度:Water: 100 mM
纯度:98%
存储:Store at -20°C
库存:现货

Background:

MRS2179 is a competitive purinergic P2Y1receptor antagonist (Kb= 102 nM).1It is selective for P2Y1over P2Y2, P2Y4, P2Y6, P2Y12, and P2Y13, as well as P2X1-4, receptors at 10 µM.2,3MRS2179 reduces phospholipase C (PLC) activity induced by the P2Y receptor agonist 2-methylthioadenosine diphosphate with an IC50value of 331 nM in turkey erythrocyte membranes that endogenously express high levels of the P2Y1receptor.1It inhibits platelet shape change and aggregation induced by ADP in washed isolated human platelets when used at a concentration of 10 µM.4MRS2179 (50 mg/kg, i.v.) prolongs the length of tail bleeding time in mice, as well as decreases platelet thrombus formation in a mouse model of iron chloride-induced arterial thrombosis.4,5


1.Nandanan, E., Camaioni, E., Jang, S.-Y., et al.Structure-activity relationships of bisphosphate nucleotide derivatives as P2Y1 receptor antagonists and partial agonistsJ. Med. Chem.42(9)1625-1638(1999) 2.von KÜgelgen, I.Pharmacological profiles of cloned mammalian P2Y-receptor subtypesPharmacol. Ther.110(3)415-432(2006) 3.Brown, S.G., King, B.F., Kim, Y.-C., et al.Activity of novel adenine nucleotide derivatives as agonists and antagonists at recombinant rat P2X receptorsDrug Dev. Res.49(4)253-259(2000) 4.Tovar, C., Higgins, B., Deo, D.D., et al.Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapyCell Cycle9(16)3364-3375(2010) 5.Lenain, N., Freund, M., LÉon, C., et al.Inhibition of localized thrombosis in P2Y1-deficient mice and rodents treated with MRS2179, a P2Y1 receptor antagonistJ. Thromb. Haemost.1(6)1144-1149(2003)