产品
编 号：F745367
分子式：C24H23F2N3O2
分子量：423.46
分子式：C24H23F2N3O2
分子量：423.46
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CAS No: 1454588-34-1
产品详情
生物活性：
Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis.
体内研究：
Protease-Activated Receptor-1 antagonist 2 (Compound 14, 1 mpk i.v. dosing, rat and monkey) inhibits PAR-1 with an IC50 of 7 nM.Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC0?24 hand Cmaxin a dose-dependent manner.Protease-Activated Receptor-1 antagonist 2 doesn’t elicit any prominent liver bioactivation or tissue toxicity signals up to an AUC of 44 μM?h.Animal Model:Rat, monkey, dog
Dosage:i.v. (3 mpk for rat, 0.3 mpk for dog and monkey), p.o (10 mpk for rat, 1 mpk for dogs and monkey)
Administration:i.v., p.o (Pharmacokinetic Analysis)
Result:Pharmacokinetic parameters. compoundFLIPR IC50 (nM)MRT (R;c D; d Me)F% (R;f D; g Mh)predicted human MRT
Protease-Activated Receptor-1 antagonist 271.9; 18; 2554; 100; 3720?48
Protease-Activated Receptor-1 antagonist 2 is an orally active protease-activated receptor-1 (PAR-1) antagonist, with an IC50 value of 7 nM. Protease-Activated Receptor-1 antagonist 2 has favorable pharmacokinetic properties which is useful in the research of cardiovascular disease (CVD), such as atherosclerosis and restenosis.
体内研究：
Protease-Activated Receptor-1 antagonist 2 (Compound 14, 1 mpk i.v. dosing, rat and monkey) inhibits PAR-1 with an IC50 of 7 nM.Protease-Activated Receptor-1 antagonist 2 (10-50 mpk, p.o., rat) increase s both the AUC0?24 hand Cmaxin a dose-dependent manner.Protease-Activated Receptor-1 antagonist 2 doesn’t elicit any prominent liver bioactivation or tissue toxicity signals up to an AUC of 44 μM?h.Animal Model:Rat, monkey, dog
Dosage:i.v. (3 mpk for rat, 0.3 mpk for dog and monkey), p.o (10 mpk for rat, 1 mpk for dogs and monkey)
Administration:i.v., p.o (Pharmacokinetic Analysis)
Result:Pharmacokinetic parameters. compoundFLIPR IC50 (nM)MRT (R;c D; d Me)F% (R;f D; g Mh)predicted human MRT
Protease-Activated Receptor-1 antagonist 271.9; 18; 2554; 100; 3720?48
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