产品
编 号：F113293
分子式：C21H27ClN8S
分子量：459.01
分子式：C21H27ClN8S
分子量：459.01
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 1303470-48-5
产品详情
生物活性：
KHK-IN-1 hydrochloride (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 hydrochloride inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 hydrochloride has potential for the study of diabetes and obesity.
体内研究：
KHK-IN-1 hydrochloride (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats.Animal Model:Male Sprague-Dawley rats (~250 g).
Dosage:10 mg/kg
Administration:Oral gavage; single
Result:Exhibited reasonable oral bioavailability in rats (F=34%; oral t1/2=4 h), but had a high volume of distribution (Vdss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).
体外研究：
KHK-IN-1 hydrochloride stable in human and rat liver microsome preparations (88 and 72% remaining at 10 min) and do not significantly inhibit cytochrome P450s from human liver microsomes (1A2, 2C19, 2D6, 2C9, and 3A4).KHK-IN-1 hydrochloride (0-10 μM; incubate 30 min, then add to 15 mM fructose and incubate for another 3 h) inhibits production of F1P in HepG2 cell lysates with an IC50 value of 400 nM.
KHK-IN-1 hydrochloride (compound 8) is a selective and cell membrane permeable ketohexokinase (KHK) inhibitor (IC50=12 nM; F=34%). KHK-IN-1 hydrochloride inhibits the production of F1P in HepG2 cell lysates (IC>sub>50=400 nM). KHK-IN-1 hydrochloride has potential for the study of diabetes and obesity.
体内研究：
KHK-IN-1 hydrochloride (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats.Animal Model:Male Sprague-Dawley rats (~250 g).
Dosage:10 mg/kg
Administration:Oral gavage; single
Result:Exhibited reasonable oral bioavailability in rats (F=34%; oral t1/2=4 h), but had a high volume of distribution (Vdss= 32 L/kg) and a high rate of clearance (CL=160 mL/min/kg).
体外研究：
KHK-IN-1 hydrochloride stable in human and rat liver microsome preparations (88 and 72% remaining at 10 min) and do not significantly inhibit cytochrome P450s from human liver microsomes (1A2, 2C19, 2D6, 2C9, and 3A4).KHK-IN-1 hydrochloride (0-10 μM; incubate 30 min, then add to 15 mM fructose and incubate for another 3 h) inhibits production of F1P in HepG2 cell lysates with an IC50 value of 400 nM.
产品资料
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