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ACT-246475

Chemical Structure : ACT-246475

CAS No.: 1159500-34-1

ACT-246475 (Selatogrel;ACT246475;ACT 246475)

Catalog No.: PC-35577Not For Human Use, Lab Use Only.

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

ACT-246475 (ACT246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.
ACT-246475 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.
ACT-246475 inhibits plateletaggregation with IC50 of 8.0 nM in the light transmission aggregometry (LTA) assay.
ACT-246475 showes efficacy in the rat ferric chloride thrombosis model when administered intravenously.

Physicochemical Properties

M.Wt 618.628
Formula C28H39N6O8P
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic acid butyl ester

References

1. Caroff E, et al. J Med Chem. 2015 Dec 10;58(23):9133-53.

2. Rey M, et al. Pharmacol Res Perspect. 2017 Oct;5(5).

3. Juif PE, et al. J Clin Pharmacol. 2018 Aug 8. doi: 10.1002/jcph.1296.

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