Canagliflozin hemihydrate

SKU: orb1706415

Description

Canagliflozin hemihydrate (TA-7284) is a selective SGLT2 inhibitor used in type 2 diabetes research. By blocking renal glucose reabsorption, it promotes significant urinary glucose excretion. This compound is widely applied in both in vitro binding assays and in vivo metabolic disease models to study glucose homeostasis and related pathways.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 928672-86-0
• MW: 907.05
• Purity: 99.96% (May vary between batches)
• 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: DMSO:255 mg/mL (281.13 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (3.64 mM)

Bioactivity

• Target IC50:
  mSGLT2/rSGLT2/hSGLT2 (CHOK cells):2/3.7/4.4 nM (IC50)
• In Vivo:
  Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice, while Canagliflozin (3 mg/kg for 3 weeks) increased urinary glucose excretion (UGE) without significant change in total food intake, resulting in decreased body weight in ZF rats.
• 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: store at low temperature | 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

Canagliflozin Hemihydrate, Canagliflozin, JNJ 28431754, JNJ-28431754, JNJ28431754, TA 7284, TA-7284, TA7284, SGLT2

Compound Identifiers

PubChem CID

24997615