KHK-IN-1 (hydrochloride)


CAS No. : 1303470-48-5

1303470-48-5
Price and Availability of CAS No. : 1303470-48-5
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Cat. No. : HY-12841A
M.Wt: 459.01
Formula: C21H27ClN8S
Purity: >98 %
Solubility: H2O : 14.29 mg/mL (ultrasonic;warming;heat to 60°C);DMSO : 25 mg/mL (ultrasonic)
Introduction of 1303470-48-5 :

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[1]. IC50 & Target:IC50=12 nM (KHK)[1]. In Vitro: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)[1].
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[1]. In Vivo:KHK-IN-1 hydrochloride (10 mg/kg; p.o.; single) shows oral bioavailability of 34% in rats[1].

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