Dapagliflozin-BMS-512148-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDapagliflozinCat. No.: HY-10450CAS No.: 461432-26-8Synonyms: BMS-512148分式: CHClO分量: 408.87作靶点: SGLT作通路: Membrane Transporter/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 m

2、g/mL (244.58 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4458 mL 12.2288 mL 24.4577 mL5 mM 0.4892 mL 2.4458 mL 4.8915 mL10 mM 0.2446 mL 1.2229 mL 2.4458 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(

3、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 (6.11 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.11 mM); Clear solution1/3 Master of Small Mol

4、ecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Dapagliflozin (BMS-512148)于治疗2型糖尿病的钠-葡萄糖共转运蛋2 (SGLT2)抑制剂。IC50 & Target SGLT2 1体外研究 Dapagliflozin pretreatment of hypoxic HK2 cells significantly improves the cell viabil

5、ity in a dose-dependentmanner. Dapagliflozin decreases Bax expression, the Bax/Bcl2 ratio, and PARP expression in hypoxic HK2cells 2.体内研究 At 11 mM glucose, dapagliflozin raises glucagon release from 18% to 32% of control, while the effect ofdapagliflozin addition is minor at 1 mM glucose. At the int

6、ermediate glucose concentration of 6 mM, glucagonsecretion is estimated to be 24% and 30% of control in the absence or presence of dapagliflozin, respectively1. Dapagliflozin pretreatment significantly reduces the number of TUNEL-positive cells in IR-injured kidneys.Dapagliflozin pretreatment signif

7、icantly elevates the HIF1 expression in IR-injured renal tubular cells frommice 2. Dapagliflozin (10 mg/kg, o.p.) causes a marked increase in urinary glucose in SGLT2i-mice.Dapagliflozin acutely suppresses BAT thermogenesis by reducing sympathetic nerve activity. Dapagliflozinenhances hepatic glucon

8、eogenesis and glycogenolysis 3.PROTOCOLCell Assay 2 To perform the cell survival assay, cells are collected after 24 h incubation with vehicle or dapagliflozinpretreatment in 30-min ischemia and surviving cells are counted with Trypan blue staining. The percentagesurvival is determined by quantizati

9、on of the relative viable number of treated cells divided by the viablenumber of untreated cells.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal 10-week-old male C57BL/6 mice weighing 30-33 g each are divided into five groups: vehicle (Vh)-treate

10、dAdministration 1 sham (n=5), dapagliflozin-treated sham (n=5), Vh-treated IR (n=7), dapagliflozin-treated IR (n=7), andalbendazole and dapagliflozin treated IR (n=7). Dapagliflozin is administrated via oral gavage at a dose of 10mg/kg/day for 2 days, starting 24 h before surgery. Albendazole is inj

11、ected subcutaneously 1 h before IRsurgery.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Mol Metab. 2019 Jan;19:1-12. Cell Physiol Biochem. 2018;45(5):1747-1758. Biochem Pharmacol. 2018 Jun;152:45-59.2/3 Master of Small Molecules 您边的抑制剂师www

12、.MedChemE Front Endocrinol. 2019 Jul. Vascul Pharmacol. 2018 Oct;109:56-71.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Pedersen MG, et al. Dapagliflozin stimulates glucagon secretion at high glucose: experiments and mathematical simulations of humanA-cells. Sci Rep. 2016 Au

13、g 18;6:31214.2. Yoon-Kyung Chang, et al. Dapagliflozin, SGLT2 Inhibitor, Attenuates Renal Ischemia-Reperfusion Injury. PLoS One. 2016; 11(7):e0158810.3. Chiba Y, et al. Dapagliflozin, a Sodium-Glucose Co-Transporter 2 Inhibitor, Acutely Reduces Energy Expenditure in BAT via NeuralSignals in Mice. PL

14、oS One. 2016 Mar 10;11(3):e0150756.4. Akahane K, et al. Efficacy of Mitiglinide Combined with Dapagliflozin in Streptozotocin-nicotinamide-induced Type 2 Diabetic Rats and inZucker Fatty Rats. Drug Res (Stuttg). 2015 Aug;65(8):416-21.5. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependentglucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 1