KHK-IN-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KHK-IN-1 是一种可逆的 ATP 竞争性酮己糖激酶 (KHK) 抑制剂，IC50 为 12 nM。在 KHK 的 ATP 结合区域中，KHK-IN-1 与 Asp-27B 相互作用。

KHK-IN-1 is a reversible and ATP-competitive inhibitor of ketohexokinase (KHK) with IC50 of 12 nM. In the ATP-binding region of KHK, KHK-IN-1 interacts with Asp-27B.

KHK-IN-1 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 (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. Cell Viability Assay Cell Line:HepG2 cells Concentration:0-10 μM Incubation Time:Incubate 30 min, then add to 15 mM fructose and incubate for another 3 h Result:Exhibited inhibition of F1P production in HepG2 cell lysates (IC50=400 nM).

KHK-IN-1 (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).

Ketohexokinase inhibitor 8 | KHK-IN-8

Others

Other Targets

GLP-1

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1303469-70-6

422.56

C21H26N8S

>98% (HPLC)

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CSc1ccccc1Nc1nc(nc2c(NCC3CC3)ncnc12)N1CCNCC1

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(-20℃)

With Ice Pack

≥ 2 years