产品
编 号：F284036
分子式：C23H24N4O5S
分子量：468.53
分子式：C23H24N4O5S
分子量：468.53
产品类型
规格
价格
是否有货
结构图
CAS No: 2299200-91-0
产品详情
生物活性：
Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders.
体内研究：
Oral antiplatelet agent 1 (2.5-80 mg/kg; p.o.; single dosage) decreases thrombus weight in FeCl3 thrombosis model rats.Oral antiplatelet agent 1 (2.5-40 mg/kg; p.o.; single dosage) prolongs the bleeding time in tail-bleeding model rats.Oral antiplatelet agent 1 exhibits great stability in both rat and human liver microsomes with the low clearance values and long half-life [human: T1/2=208.3 min, Clint=10.1 mL/(min g protein); rats: T1/2=89.1 min, Clint=10.6 mL/(min g protein)].Oral antiplatelet agent 1 (5 mg/kg; p.o.; single dosage) exhibits excellent pharmacokinetic properties with relatively low clearance, high plasma exposure and good oral bioavailability in rats.Animal Model:Male Wistar rats (250-300 g, n = 10; FeCl3 thrombosis model)
Dosage:2.5, 5, 10, 20, 40 and 80 mg/kg
Administration:p.o.; single dosage
Result:Decreased thrombus weight in a dose-dependent manner with an ED50 of 27 mg/kg compared to that of 7 mg/kg for Clopidogrel (HY-15283).
Animal Model:Male rats (250-300 g, n = 10; tail-bleeding model)
Dosage:2.5, 5, 10, 20 and 40 mg/kg
Administration:p.o.; single dosage
Result:Prolonged the bleeding time in a dose-dependent manner.
Animal Model:Male Sprague-Dawley rats (200-220g)
Dosage:5 mg/kg
Administration:p.o.; single dosage
Result:Pharmacokinetic Parameters of Oral antiplatelet agent 1 (compound 58l) in male Sprague-Dawley rats.Cmax (ng/mL) T1/2 (h) Tmax (h) AUC0-∞ (ng·h/mL) MRT (h)
p.o. 5 mg/kg1661 ± 6422.91 ± 1.090.254120 ± 21273.64 ± 0.18
体外研究：
Oral antiplatelet agent 1 (compound 58l) moderately inhibits CYP3A4 with an IC50 of about 1.5 μM, but exhibits weak inhibition in the other main subtypes (IC50>25 μM).Oral antiplatelet agent 1 does not inhibit hERG even at 40 μM, indicating that it has no QT interval prolongation-related cardiac toxicity.
Oral antiplatelet agent 1 is a potent P2Y12 receptor antagonist. Oral antiplatelet agent 1 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. Oral antiplatelet agent 1 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. Oral antiplatelet agent 1 can be used to research thromboembolic disorders.
体内研究：
Oral antiplatelet agent 1 (2.5-80 mg/kg; p.o.; single dosage) decreases thrombus weight in FeCl3 thrombosis model rats.Oral antiplatelet agent 1 (2.5-40 mg/kg; p.o.; single dosage) prolongs the bleeding time in tail-bleeding model rats.Oral antiplatelet agent 1 exhibits great stability in both rat and human liver microsomes with the low clearance values and long half-life [human: T1/2=208.3 min, Clint=10.1 mL/(min g protein); rats: T1/2=89.1 min, Clint=10.6 mL/(min g protein)].Oral antiplatelet agent 1 (5 mg/kg; p.o.; single dosage) exhibits excellent pharmacokinetic properties with relatively low clearance, high plasma exposure and good oral bioavailability in rats.Animal Model:Male Wistar rats (250-300 g, n = 10; FeCl3 thrombosis model)
Dosage:2.5, 5, 10, 20, 40 and 80 mg/kg
Administration:p.o.; single dosage
Result:Decreased thrombus weight in a dose-dependent manner with an ED50 of 27 mg/kg compared to that of 7 mg/kg for Clopidogrel (HY-15283).
Animal Model:Male rats (250-300 g, n = 10; tail-bleeding model)
Dosage:2.5, 5, 10, 20 and 40 mg/kg
Administration:p.o.; single dosage
Result:Prolonged the bleeding time in a dose-dependent manner.
Animal Model:Male Sprague-Dawley rats (200-220g)
Dosage:5 mg/kg
Administration:p.o.; single dosage
Result:Pharmacokinetic Parameters of Oral antiplatelet agent 1 (compound 58l) in male Sprague-Dawley rats.Cmax (ng/mL) T1/2 (h) Tmax (h) AUC0-∞ (ng·h/mL) MRT (h)
p.o. 5 mg/kg1661 ± 6422.91 ± 1.090.254120 ± 21273.64 ± 0.18
体外研究：
Oral antiplatelet agent 1 (compound 58l) moderately inhibits CYP3A4 with an IC50 of about 1.5 μM, but exhibits weak inhibition in the other main subtypes (IC50>25 μM).Oral antiplatelet agent 1 does not inhibit hERG even at 40 μM, indicating that it has no QT interval prolongation-related cardiac toxicity.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备