产品
编 号：F742793
分子式：C20H18F6N2O
分子量：416.36
分子式：C20H18F6N2O
分子量：416.36
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CAS No: 1159997-27-9
产品详情
生物活性：
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.
体内研究：
AMG9678 (0-100 mg/kg; p.o.; once) produces a significant and somewhat dose-dependent decrease in body temperature (Tb) in rats.AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing in rats.Animal Model:Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age)
Dosage:10, 30 and 100 mg/kg
Administration:Oral administration, once or once daily for 4 consecutive days
Result:Produced a significant and somewhat dose-dependent decrease in Tb at 10, 30 and 100 mg/kg. The magnitude of TRPM8 blockade-induced decrease in body temperature is reduced after repeated dosing.Effect of AMG9678 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCTCompoundDose mg/kg (route) Max Tb decrease (°C) P value * Time post dosing (min) Plasma concentration
AMG967810 (p.o.)0.72p < 0.001600.04 ± 0.006
AMG967830 (p.o.)0.70p < 0.01600.34 ± 0.1
AMG9678100 (p.o.)0.83p < 0.05600.36 ± 0.12
体外研究：
AMG9678 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 7.6 h.
AMG9678 is a potent, selective, orally active antagonist of TRPM8 with an IC50 of 31.2 nM.
体内研究：
AMG9678 (0-100 mg/kg; p.o.; once) produces a significant and somewhat dose-dependent decrease in body temperature (Tb) in rats.AMG9678 (30 mg/kg; p.o.; once daily for 4 consecutive days) decreases reduced body temperature after repeated dosing in rats.Animal Model:Male Sprague Dawley rats weighing 200–350 g (6–12 weeks of age)
Dosage:10, 30 and 100 mg/kg
Administration:Oral administration, once or once daily for 4 consecutive days
Result:Produced a significant and somewhat dose-dependent decrease in Tb at 10, 30 and 100 mg/kg. The magnitude of TRPM8 blockade-induced decrease in body temperature is reduced after repeated dosing.Effect of AMG9678 on Tb in rats. P value is for comparing compound administered rat Tb with vehicle administered rat Tb. End of the study plasma concentration is reported in μM. Asterisk indicates one-way ANOVA followed by Dunnett's MCTCompoundDose mg/kg (route) Max Tb decrease (°C) P value * Time post dosing (min) Plasma concentration
AMG967810 (p.o.)0.72p < 0.001600.04 ± 0.006
AMG967830 (p.o.)0.70p < 0.01600.34 ± 0.1
AMG9678100 (p.o.)0.83p < 0.05600.36 ± 0.12
体外研究：
AMG9678 potently inhibits the menthol and cold-induced increase in intracellular calcium in cells expressing rat TRPM8, the plasma half-life (T1/2) in rats is 7.6 h.
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