| 产品描述： | 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 |
| 靶点： |
IC50=12 nM (KHK);Others |
| 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. 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). |
| 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). |
| 参考文献： |
1. Maryanoff BE, et al. Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site. ACS Med Chem Lett. 2011 Apr 18;2(7):538-43. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.179 ml |
10.893 ml |
21.786 ml |
| 5 mM |
0.436 ml |
2.179 ml |
4.357 ml |
| 10 mM |
0.218 ml |
1.089 ml |
2.179 ml |
| 50 mM |
0.044 ml |
0.218 ml |
0.436 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京