Dapagliflozin (BMS-512148) - Moligand™, 10mM in DMSO , Inhibitor of Sodium/glucose cotransporter 1;Inhibitor of Sodium/glucose cotransporter 2, CAS No.461432-26-8, Inhibitor of Sodium/glucose cotransporter 1;Inhibitor of Sodium/glucose cotransporter 2

CAS: 461432-26-8 Cat. No.: D408687 Peso molecular: 408.87 Número EC: 639-683-0

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

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%

Specifications

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Dapagliflozin (BMS-512148) is a potent and selective hSGLT2 inhibitor with EC50 of 1.1 nM, exhibiting 1200-fold selectivity over hSGLT1. Phase 4.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of Sodium/glucose cotransporter 1;Inhibitor of Sodium/glucose cotransporter 2

Nombres e identificadores

• Isómeros 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
• Peso molecular: 408.87
• Reaxy-Rn: 21800523
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21800523&ln=

Objetivos asociados (humanos)

SLC5A4 Tchem Solute carrier family 5 member 4 (1 Activities)

Discover Target: SLC5A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC5A11 Tchem Sodium/myo-inositol cotransporter 2 (1 Activities)

Discover Target: SLC5A11

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC5A2 Tclin Sodium/glucose cotransporter 2 (37 Activities)

Discover Target: SLC5A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC5A1 Tclin Sodium/glucose cotransporter 1 (15 Activities)

Discover Target: SLC5A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

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

Referencias

1. Zhonghua Dong, Xiao Li, Xuan Wang, Jingya Xu, Wei Xu.  (2025)  Ergosterol from Edible Fungi: Enhancing Fatty Acid Oxidation via CPT1A to Protect Against Diabetic Kidney Disease.  Food & Function,      [PMID:40704985] [10.1039/D5FO00371G]

2. Wenyu Du, Zihan Liu, Zhi Wang, Xin Zhou, Zhanjun Dong, Ying Li.  (2025)  In vivo assessment of pharmacokinetic interactions of empagliflozin and henagliflozin with sorafenib: an animal-based study.  PeerJ,      [PMID:40656939] [10.7717/peerj.19662]

3. Qin Fei, Zeng Huicong, Zhou Li, Zhou Zhenhua, Mao Yongxin, Zeng Youyan, Guo Rongxiang, Chen Kaixian, Zhao Dongyu, Yao Weiwei, Zhang Bin, Zhou Qian, Li Bo.  (2025)  Identification of novel small molecules as potential SGLT2 inhibitors through combined virtual screening and experimental validation.  MOLECULAR DIVERSITY,      [PMID:41021175] [10.1007/s11030-025-11367-4]

4. Xueru He, Ying Li, Yajing Li, Caihui Guo, Yuhao Fu, Xuejiao Xun, Zhi Wang, Zhanjun Dong.  (2023)  In vivo assessment of the pharmacokinetic interactions between donafenib and dapagliflozin, donafenib and canagliflozin in rats.  BIOMEDICINE & PHARMACOTHERAPY,      [PMID:37027985] [10.1016/j.biopha.2023.114663]

5. Shuo Zhang, Shuang Guo, Pengyu Wang, Yan Song, Leiming Yang, Qiyu Sun, Qi Huang, Youzhi Zhang.  (2025)  Dapagliflozin attenuates skeletal muscle atrophy in diabetic nephropathy mice through suppressing Gasdermin D-mediated pyroptosis.  INTERNATIONAL IMMUNOPHARMACOLOGY,      [PMID:39837016] [10.1016/j.intimp.2025.114088]

6. Wan Zhijie, Yuan Ming, Liu Ziao, Cai Yuan, He Hua, Hao Kun.  (2025)  Impact of Dapagliflozin on Hepatic Lipid Metabolism and a Dynamic Model of Ketone Body Levels.  AAPS Journal,  27  (1): (1-14).  [PMID:39900889] [10.1208/s12248-025-01024-x]

7. Wanxian Wang, Yanfang Liu, Dian Liu, Han Zhou, Yan Li, Wenjie Yuan, Suowen Xu, Jixia Wang, Xinmiao Liang, Jianping Weng.  (2024)  Profiling of Antidiabetic Bioactive Flavonoid Compounds from an Edible Plant Kudzu (Pueraria lobata).  JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,      [PMID:38976778] [10.1021/acs.jafc.4c02564]

8. Pengyu Wang, Zhen Sun, Qing Lan, Shuo Zhang, Yan Song, Leiming Yang, Mi Chen, Jianfen Shen, Qi Huang, Youzhi Zhang.  (2025)  Bioinformatics analysis combined with experimental validation reveals the novel mechanisms of multi-targets of dapagliflozin attenuating diabetic liver injury.  Frontiers in Endocrinology,      [PMID:40438398] [10.3389/fendo.2025.1519153]

9. Xiaoming Zou, Baoyin Zhang, Yujiao Jing, Lihui Zong, Ligui Wu, Qunyan Zhou, Yue Fang, Kaifang Shen, Xubiao Luo, Lingling Rong.  (2025)  Significant effects of electrophilicity in oral antidiabetic drugs upon conjugative transfer of drug-resistance plasmids in activated sludge and the mechanisms.  WATER RESEARCH,      [PMID:41442951] [10.1016/j.watres.2025.125250]

10. Qi Wu, Yupeng Tao, Chenchen Sun, Yijing Li, Tianyu Liu, Buhui Liu, Wei Li, Kun Gao, Yao Zhou.  (2026)  Isoquercitrin Improves Renal Tubular Epithelial Cell Mitochondrial Dysfunction by Regulating Extracellular Signal-Regulated Kinase/Reactive Oxygen Species Signaling and Connexin 43 Expression in Diabetic Kidney Disease.  PHYTOTHERAPY RESEARCH,      [PMID:] [10.1002/ptr.70307]