Dapagliflozin-BMS-512148-DataSheet-生命科學試劑-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作靶點: SGLT作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 m

2、g/mL (244.58 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據產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。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(

3、為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存條件，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: 2.5 mg/mL (6.11 mM); Clear solution2. 請依序添加每種溶劑： 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 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.11 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Dapagliflozin (BMS-512148)于治療2型糖尿病的鈉-葡萄糖共轉運蛋2 (SGLT2)抑制劑。IC50 & Target SGLT2 1體外研究 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.體內研究 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.戶使本產品發(fā)表的科研獻 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 您邊的抑制劑師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