Dapagliflozin (BMS-512148) is a potent and selectivehSGLT2inhibitor withEC50of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.
In vitro

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

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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

规格

英文别名

(2S,3R,4R,5S,6R)-2-(3-(4-ethoxybenzyl)-4-chlorophenyl)-6-(hydroxymethyl)-tetrahydro-2H-pyran-3,4,5-triol

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Dapagliflozin (BMS-512148)

生化机理

Dapagliflozin（BMS-512148）是一种强效的选择性 hSGLT2 抑制剂，EC50 为 1.1 nM，与 hSGLT1 相比具有 1200 倍的选择性。第 4 阶段

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

钠/葡萄糖共转运体 1 抑制剂；钠/葡萄糖共转运体 2 抑制剂

名称和识别符

EC号

639-683-0

分子类型

小分子

Isomeric SMILES

CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)[C@H]3[C@@H]([C@H]([C@@H]([C@H](O3)CO)O)O)O)Cl

分子量

408.87

Reaxy-Rn

21800523

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21800523&ln=

技术文档

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高级数据

关联靶点（人）

SLC5A4 Tchem 溶质载体家族 5 成员 4(Solute carrier family 5 member 4) (1 活性数据)

点击查看靶蛋白信息： SLC5A4

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

SLC5A11 Tchem 钠/肌醇协同转运蛋白 2(Sodium/myo-inositol cotransporter 2) (1 活性数据)

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活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

SLC5A2 Tclin 钠/葡萄糖协同转运蛋白 2(Sodium/glucose cotransporter 2) (37 活性数据)

点击查看靶蛋白信息： SLC5A2

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

SLC5A1 Tclin 钠/葡萄糖协同转运蛋白 1(Sodium/glucose cotransporter 1) (15 活性数据)

点击查看靶蛋白信息： SLC5A1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro Water: 6 mg/mL (40.21 mM); DMSO: Insoluble;

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批号(Lot Number)	证书类型	货号
L2205207	分析证书	D408687

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