product name ML161
Description: ML-161 is a potent allosteric inhibitor of PAR1 with IC50 of 0.26 μM. ML161 has a different selectivity with the reported ALK inhibitor crizotinib. When tested with human platelets, ML161 treatment inhibited the activation of thrombin-induced platelet in a dose-dependent manner by detecting P-selectin expression. When tested with granule secretion, ML161 exhibited a potent inhibition on P-selectin expression in a dose-dependent manner with EC50 value of 0.3μM and also inhibited SFLLRN-induced thrombus formation.
References: ACS Med Chem Lett. 2012 Mar 8;3(3):232-237.
361.23
Formula
C17H17BrN2O2
CAS No.
423735-93-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 72 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: ML-161 is an allosteric inhibitor of PAR1. 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Med Chem Lett. 2012 Mar 8;3(3):232-237. |
