MRS 2395

Names

[ Name ]:
MRS 2395

[Synonym ]:
2,2-dimethyl-propionic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethyl-propionyloxymethyl)-propyl ester
2,2-dimethyl-propanoic acid 3-(2-chloro-6-methylaminopurin-9-yl)-2-(2,2-dimethyl-propionyloxymethyl)-propyl ester
mrs 2395

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> P2Y Receptor

[References]

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₃₀ClN₅O₄

[ Molecular Weight ]:
439.93600

[ Exact Mass ]:
439.19900

[ PSA ]:
108.23000

[ LogP ]:
3.38920

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation.

J. Med. Chem. 45 , 5694-5709, (2002)

Activation by ADP of both P2Y(1) and P2Y(12) receptors in platelets contributes to platelet aggregation, and antagonists at these receptor subtypes have antithrombotic properties. In an earlier public...