ACT-246475 | P2Y12 antagonist | Probechem Biochemicals

Chemical Structure : ACT-246475

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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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.

ACT-246475 (Selatogrel, ACT246475, ACT 246475)

Biological Activity

Physicochemical Properties

References

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