Ketohexokinase-inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKetohexokinase inhibitor 1Cat. No.: HY-U00461CAS No.: 2102501-84-6分式: CHFNO分量: 356.34作靶点: Others作通路: Others储存式: 4C, sealed storage, away from moisture* In solvent : -80C, 6 months; -20C, 1 month (sealedstorage, away from moistur

2、e)溶解性数据体外实验 DMS : 125 mg/mL (350.79 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.8063 mL 14.0315 mL 28.0631 mL5 mM 0.5613 mL 2.8063 mL 5.6126 mL10 mM 0.2806 mL 1.4032 mL 2.8063 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案

3、，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.84 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.84 mM); Clear solut

4、ion3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.84 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Ketohexokinase inhibitor 1种酮糖激酶 (ketohexokinase (KHK) 抑制剂，对 KHK-C 和 KHK-A 的 IC50值分别为 8.4 nM 和 66 nM，摘专利 US 20170183328 A1，example 4。IC50 & Tar

5、get IC50: 8.4 nM (KHK-C), 66 nM (KHK-A) 1体外研究 Ketohexokinase inhibitor 1 (Example 4) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66nM for KHK-C and KHK-A, sepctively 1.PROTOCOLKinase Assay 1 A 384-well format on a assay plate is used in the assay and monitored by UV-vis spectro

6、scopy in continuousmode at room temperature (rt). Compounds (Ketohexokinase inhibitor 1) are prepared in DMSO as 4 mMstocks, diluted using an 11-point half-log scheme on a Biomek FX, and incubated at rt for 30 minutes with thereaction mixture containing 50 mM HEPES, pH 7.4, 140 mM KCl, 3.5 mM MgCl2,

7、 0.8 mM fructose, 2 mMTCEP, 0.8 mM PEP, 0.7 mM NADH, 0.01% Triton X-100, 30 U/mL pyruvate kinase-lactate dehydrogenase,and 10 nM purified KHK-C. The compound concentration in each well ranged from 1 nM to 100 M. Thereaction is initiated with the addition of 0.2 mM ATP. The absorbance is measured for

8、 30 minutes on aSpectraMax reader after ATP is added. The concentrations provided are based on the final mixture volume of40 L 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. SUBSTITUTED 3-AZABICYCLO3.1.0HEXANES AS KETOHEXOKINASE INHIBITORS. US 20170183328 A1McePdfHeightCaution: Product has not been fully validated for medical application