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KI3746ML16110 mg$250
ML16150 mg$800

Chemical Characteristic

Product NameML161
CAS No.423735-93-7
Molecular Weight 361.23
FormulaC17H17BrN2O2
SmilesC(=O)(c1c(cccc1)Br)Nc1cc(ccc1)NC(=O)CCC
Chemical Structure

Biological activities

ML-161 is an allosteric inhibitor of PAR1 with IC50 0.26?M. ML-161 displays dose-dependent inhibition of thrombin-induced platelet activation, as measured by P-selectin expression. ML-161 displays selective inhibition of SFLLRN and thrombin-induced platelet aggregation, both of which operate via PAR1, and has no effect on AYPGKF, thromboxane, or ADP-induced platelet aggregation, which are all agonists at alternative platelet GPCRs [1].

References

[1] Dockendorff C, Aisiku O, Verplank L, et al. Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor. ACS Med Chem Lett. 2012,3(3):232-237.

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