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  • Dapagliflozin

    • 达格列净;达格列嗪;BMS-512148
    货号: abs813289
    CAS号: 461432-26-8
    分子式: C21H25ClO6
    分子量: 408.87
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    货号-规格 货期 价格 数量
    abs813289-5mg 现货 ¥798.00
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    abs813289-10mg 现货 ¥1161.00
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    abs813289-50mg 现货 ¥2787.00
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    大包装询价
    产品描述
    描述

    Dapagliflozin是一种有效的,选择性的hSGLT2抑制剂,EC50为1.1 nM,比作用于hSGLT1选择性高1200倍。Dapagliflozin对hSGLT1不敏感,IC50是hSGLT2的1200倍。 Dapagliflozin作用于hSGLT2比Phlorizin效果高32倍。作用于hSGLT1比Phlorizin效果低4倍。

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    达格列净;达格列嗪;BMS-512148
    外观
    White to off-white solid
    可溶性/溶解性
    DMSO : ≥ 100 mg/mL (244.58 mM)
    生物活性
    靶点
    hSGLT2
    In vitro(体外研究)
    Dapagliflozin is not sensitive to hSGLT1 with a 1200-fold IC50. Dapagliflozin is 32-fold more potent than phlorizin against hSGLT2 but 4-fold less than phlorizin against hSGLT1. Dapagliflozin is highly selective versus GLUT transporters and displays 8–9% inhibition in protein-free buffer at 20 μM and virtually no inhibition in the presence of 4% bovine serum albumin. Dapagliflozin has good permeability across Caco-2 cell membranes and is a substrate for P-glycoprotein (P-gp) but not a significant P-gp inhibitor. Dapagliflozin is stable in rat, dog, monkey, and human serum at 10 μM. Dapagliflozin shows no inhibitory responses or induction to human P450 enzymes. The in vitro metabolic pathways Dapagliflozin are glucuronidation, hydroxylation, and O-deethylation.
    In vivo(体内研究)
    Dapagliflozin reduces blood glucose levels by 55% after 0.1 mg/kg oral dose in hyperglycemic streptozotocin (STZ) rats, which is in part to the metabolic stability conferred by the C-glucoside linkage. Dapagliflozin displays a favorable absorption, distribution, metabolism, and excretion (ADME) profile and is orally bioavailable. Dapagliflozin (1 mg/kg) causes significant dose-dependent glucosuria and increase in urine volume in normal rats over 24 hours post-dose. Dapagliflozin induces increase in urine glucose and urine volume excretion at 6 hours post-dose in Zucker diabetic fatty (ZDF) rats. Dapagliflozin lowers fasting and fed glucose levels in ZDF rats even by 2 weeks of treatment, without any marker of renal or liver toxicity. Dapagliflozin significantly reduces the development of hyperglycaemia, with lowered blood glucose. Dapagliflozin could improve the insulin sensitivity, reduce β-cell mass and the development of impaired pancreatic function.
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