Canagliflozin-hemihydrate-JNJ-24831754ZAE-hemihydrate-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECanagliflozin hemihydrateCat. No.: HY-I0383CAS No.: 928672-86-0Synonyms: JNJ 24831754ZAE (hemihydrate); JNJ 28431754(hemihydrate); JNJ 28431754AAA (hemihydrate); TA 7284(hemihydrate)分式: CHFO.S分量: 453.52作靶点: SGLT作通路: Membrane Tra

2、nsporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (220.50 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2050 mL 11.0249 mL 22.0497 mL5 mM 0.4410 mL 2.2050 mL 4.4099 mL10 mM 0.2205 mL

3、1.1025 mL 2.2050 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，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: 2.5 mg/mL (5.51 mM); Clear solution1/3 Mas

4、ter of Small Molecules 您边的抑制剂师www.MedChemE2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.51 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.51 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Canagliflozin hemihydrate (JNJ28431754 hemihydrate; TA-72

5、84 hemihydrate)种选择性的 SGLT2 抑制剂，作于表达 mSGLT2，rSGLT2 和 hSGLT2 的 CHO细胞，IC50 分别为 2 nM，3.7 nM 和 4.4 nM 1。IC50 & Target IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells) 1体外研究 Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.41.2 nM.Similar IC50 values are o

6、btained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat andmouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cellswith IC50 of 684159 nM and 1,000 nM, respectively 1.体内研究 Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (

7、BG) levels, respiratory exchangeratio, and body weight gain in DIO mice 1.Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change intotal food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats1.Animal M

8、odel: Diet-induced obese, insulin resistantmice (DIO) Mice 1Dosage: 30 mg/kgAdministration: Oral gavage; daily; 4 weeksResult: Reduced BG levels, respiratory exchange ratio, and body weight gain.Animal Model: Male Zucker fatty (ZF) obese, insulin resistant rats 1Dosage: 3 mg/kgAdministration: Oral g

9、avage; daily; 3 weeksResult: UGE was increased with no significant change in total food intake compared with that invehicle-treated rats, leading to a decrease in body weight.户使本产品发表的科研献 Nature. 2018 Aug;560(7719):499-503. Mol Metab. 2019 Jan;19:1-12.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE

10、 Biochem Pharmacol. 2018 Jun;152:45-59. Vascul Pharmacol. 2018 Oct;109:56-71. Int J Med Sci. 2018 Jun 13;15(9):937-943.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animalmodels.PLoS One. 2012;7(2):e30555.McePdfHeightCaution: Product has not been fully v