Canagliflozin hemihydrate

SKU: orb2901577

Description

Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC50s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 928672-86-0
• MW: 907.05
• Purity: >98% (HPLC)
• Formula: C₄₈H₅₂F₂O₁₁S₂
• SMILES: O[C@H]1[C@H](C2=CC(CC3=CC=C(C4=CC=C(C=C4)F)S3)=C(C=C2)C)O[C@@H]([C@H]([C@@H]1O)O)CO.O[C@H]5[C@H](C6=CC(CC7=CC=C(C8=CC=C(C=C8)F)S7)=C(C=C6)C)O[C@@H]([C@H]([C@@H]5O)O)CO.O
• Target: SGLT
• Solubility: In Vitro: DMSO : ≥ 100 mg/mL (220.50 mM)

Bioactivity

• In Vivo:
  Canagliflozin (30 mg/kg treatment for 4 weeks) reduces blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice. Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats. Animal model: Diet-induced obese, insulin resistantmice (DIO) Mice. Dosage: 30 mg/kg. Administration: Oral gavage; daily; 4 weeks. Result: Reduced BG levels, respiratory exchange ratio, and body weight gain. Animal model: Male Zucker fatty (ZF) obese, insulin resistant rats. Dosage: 3 mg/kg. Administration: Oral gavage; daily; 3 weeks. Result: UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.
• In Vitro:
  Canagliflozin inhibits Na+-dependent 14C-AMG uptake in CHO-hSGLT2 cells, with an IC50 of 4.4 ± 1.2 nM. Similar IC50 values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC50 = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits 14C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC50 of 684 ± 159 nM and > 1, 000 nM, respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

SGLT