ACT-246475|ACT246475;ACT 246475

Cas No.:	1159500-34-1
Chemical Name:	4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic acid butyl ester
Synonyms:	ACT246475;ACT 246475
SMILES:	N(C(OCCCC)=O)1CCN(C([C@H](NC(C2C=C(N3CC[C@@H](OC)C3)N=C(C3=CC=CC=C3)N=2)=O)CP(O)(O)=O)=O)CC1
Formula:	C₂₈H₃₉N₆O₈P
M.Wt:	618.628
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM; displays no agonist binding activity against P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, and P2Y13 at 10 uM, to P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, no antagonistic activity on P2X1, P2X2, P2X3, P2X4, and P2X7 receptors, as well as a broad panel of receptors, transporters, and enzymes; inhibits plateletaggregation with IC50 of 8.0 nM in the light transmission aggregometry (LTA) assay; showes efficacy in the rat ferric chloride thrombosis model when administered intravenously.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47245	PSB-0739	PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect.
DC46852	2-Methylthio-AMP diTEA	2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation.
DC46517	MRS2768 tetrasodium salt	MRS2768 tetrasodium salt is a moderately potent and selective P2Y2 receptor agonist. MRS2768 tetrasodium salt has a protective effect on cardiomyocytes from ischemic damage in vivo and in vitro.
DC45186	MRS2279	MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05).
DC45185	Denufosol tetrasodium	Denufosol tetrasodium (INS37217) is a long-acting P2Y2 receptor agonist, which exhibits an EC50 of ~10 μM for P2Y2 receptor activation.
DC41482	Adenosine 2',5'-diphosphate sodium	Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors.
DC40026	MRS2179 tetrasodium hydrate	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. MRS2179 tetrasodium hydrate inhibits platelet aggregation.
DC28262	PSB-1114 tetrasodium	PSB-1114 tetrasodium is a potent, enzymatically stable, and subtype-selective P2Y2 receptor agonist with an EC50 of 134 nM. PSB-1114 tetrasodium displays >50-fold selectivity versus the P2Y4 (EC50 of 9.3 μM) and P2Y6 (EC50 of 7.0 μM) receptors.
DC28245	NF157	NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
DC28244	NF546	NF546 is a selective non-nucleotide P2Y11 agonist with a pEC50 of 6.27. NF546 stimulates release of interleukin-8 from human monocyte-derived dendritic cells.