Dapagliflozin

SKU: orb1305553

Description

Dapagliflozin (BMS-512148) is a selective SGLT2 inhibitor used in type 2 diabetes research. By competitively blocking renal glucose reabsorption, it promotes glucosuria and lowers blood glucose. This mechanism is studied in vitro and in vivo for metabolic disease and cardiovascular research applications.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 461432-26-8
• MW: 408.87
• Purity: 99.93%
• Formula: C₂₁H₂₅ClO₆
• SMILES: O[C@H]1[C@@H](O[C@H](CO)[C@@H](O)[C@@H]1O)C2=CC(CC3=CC=C(OCC)C=C3)=C(Cl)C=C2
• Target: HIF,SGLT
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:4.5 mg/mL (11.01 mM);Ethanol:14 mg/mL (34.24 mM);DMSO:247.5 mg/mL (605.33 mM)

Bioactivity

• Target IC50:
  SGLT2 (human):1.1 nM (EC50)|PANC1 cells viability:435.7 μM (48h)|A549 cells viability:287.5 μM (48h)|Caco-2 cells viability:167.8 μM (48h)|Du-145 cells viability:290.1 μM (48h)|MCF-7 cells viability:243.4 μM (48h)
• In Vivo:
  METHODS: To investigate the effects on diabetic atherosclerosis, Dapagliflozin (1 mg/kg) was administered by gavage to diabetic ApoE-/- mice with high-fat diet-induced atherosclerosis once daily for 12 weeks. RESULTS: Dapagliflozin may have therapeutic potential for high-fat diet-induced diabetic atherosclerosis, and these benefits may depend on the inhibition of IL-1β secretion by macrophages via the ROS-NLRP3-caspase-1 pathway.
• In Vitro:
  METHODS: The human proximal tubule epithelial cell line HK2 was treated with Dapagliflozin (1-10 µM) under normoxic and hypoxic conditions for 24 h. Cell viability was assayed using Trypan blue staining. RESULTS: Dapagliflozin pretreatment had no effect on cell survival of normoxic HK2 cells. Hypoxia significantly reduced the cell viability of HK2 cells compared to control cells, and Dapagliflozin pretreatment of hypoxic HK2 cells significantly increased cell viability in a dose-dependent manner. METHODS: The human proximal tubule epithelial cell line HK2 was treated with Dapagliflozin (0.1 µM) and H2O2 (200 µM) for 24 h. Apoptosis was detected using Hoechst 33342 and PI. RESULTS: Dapagliflozin significantly reduced the percentage of apoptotic cell death induced by H2O2.Dapagliflozin had a protective effect against H2O2-induced cell death.
• Cell Research:
  To perform the cell survival assay, cells are collected after 24 h incubation with vehicle or dapagliflozin pretreatment in 30-min ischemia and surviving cells are counted with Trypan blue staining. The percentage survival is determined by quantization of the relative viable number of treated cells divided by the viable number of untreated cells.

Storage & Handling

• Storage: store under nitrogen,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Sodium-dependent glucose cotransporters, SGLT, hSGLT2, Inhibitor, HIF1, inhibit, Dapagliflozin, BMS512148, BMS-512148, BMS 512148

Compound Identifiers

PubChem CID

9887712