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作靶點: Others作通路: Others儲存式: 4C, sealed storage, away from moisture* In solvent : -80C, 6 months; -20C, 1 month (sealedstorage, away from moistur

2、e)溶解性數(shù)據(jù)體外實驗 DMS : 125 mg/mL (350.79 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?/p>

3、，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.84 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (5.84 mM); Clear solut

4、ion3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.84 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Ketohexokinase inhibitor 1種酮糖激酶 (ketohexokinase (KHK) 抑制劑，對 KHK-C 和 KHK-A 的 IC50值分別為 8.4 nM 和 66 nM，摘專利 US 20170183328 A1，example 4。IC50 & Tar

5、get IC50: 8.4 nM (KHK-C), 66 nM (KHK-A) 1體外研究 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