CAS NO: | 461432-26-8 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
100mg | 电议 |
Cas No. | 461432-26-8 |
别名 | 达格列净; BMS-512148 |
化学名 | (2S,3R,4R,5S,6R)-2-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol |
Canonical SMILES | CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C3C(C(C(C(O3)CO)O)O)O)Cl |
分子式 | C21H25ClO6 |
分子量 | 408.87 |
溶解度 | ≥ 15.1mg/mL in DMSO, ≥ 116.6 mg/mL in EtOH |
储存条件 | Store at-20°C,sealed storage, away from moisture |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
文献引用 | |
产品描述 | EC50: 1.1±0.06 nM for hSGLT2 Selective inhibition of SGLT2 has been proposed to aid in the normalization of plasma glucose levels in patients with diabetes by preventing the renal glucose reabsorption process and promoting glucose excretion in urine. Dapagliflozin is a potent, selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) inhibitor. In vitro: EC50 values of 1.1 nM for hSGLT2 and 1.4 μM for hSGLT1 determined for Dapagliflozin corresponded to 1200-fold selectivity for SGLT2 as compared with phlorizin’s 10-fold selectivity. Dapagliflozin inhibitory potencies against rat SGLT (rSGLT)2 and hSGLT2 were comparable, but the selectivity of Dapagliflozin for rSGLT2 versus rSGLT1 decreased to 200-fold [1]. In vivo: In vivo, dapagliflozin acutely induced renal glucose excretion in diabetic and normal rats, improved glucose tolerance in normal rats, as well as reduced hyperglycemia in Zucker diabetic fatty rats after single oral doses ranging between 0.1 and 1.0 mg/kg [2]. Clinical trial: Dapagliflozin dosing at 1, 2.5 and 5 mg/day is effective in reducing glycaemic levels and body weight in treatment-naive patients with type 2 diabetes. Dapagliflozin was well tolerated [3]. References: |