491611-55-3
Chemical Structure
MRS2395
- CAS No.: 491611-55-3
- Formula:C20H30ClN5O4
- Molecular Weight:439.94
IUPAC Name: 2-((2-chloro-6-(methylamino)-9H-purin-9-yl)methyl)propane-1,3-diyl bis(2,2-dimethylpropanoate)
InChIKey: NASABYJQIYJDID-UHFFFAOYSA-N
SMILES: CNC1=C2N=CN(CC(COC(C(C)(C)C)=O)COC(C(C)(C)C)=O)C2=NC(Cl)=N1
Biological Activity: MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6[1][2].
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MRS2395 | MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6. | |||||||||||||||||||||
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- [1]. Bin Xu, et al.Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation. J Med Chem. 2002 Dec 19;45(26):5694-709. [Content Brief]
- [2]. Annachiara Mitrugno, et al. Potentiation of TRAP-6-induced platelet dense granule release by blockade of P2Y 12 signaling with MRS2395. Platelets. 2018 Jun;29(4):383-394. [Content Brief]
Keywords
