BMS-903452

SKU: orb1741434

Description

BMS-903452 is a potent and selective GPR119 agonist (EC50 = 14 nM) for research in diabetes. It is suitable for in vivo rodent models and in vitro studies, as it shows no significant CYP450 inhibition, PXR activation, or hepatotoxicity in HepG2 cells.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1339944-47-6
• MW: 513.37
• Purity: >99.99% (May vary between batches)
• Formula: C₂₁H₁₉Cl₂FN₄O₄S
• SMILES: O=C1N(C=C(Cl)C(OC2CCN(CC2)C=3N=CC(Cl)=CN3)=C1)C4=C(F)C=C(S(C)(=O)=O)C=C4
• Target: GPCR
• Solubility: DMSO:10 mg/mL (19.48 mM)

Bioactivity

• Target IC50:
  GPR119:14nM(EC50)
• In Vivo:
  An oral glucose tolerance test (OGTT) to measure the acute efficacy of this agonist in C57/BL6 mice. Glucose excursion was 37%-40% lower in mice treated with BMS-903452 (0.1, 0.3, and 1 mg/kg) than in control mice. Treatment of SD rats with 0.3 mg/kg BMS-903452 stimulated GLP-1 production, and co-administration of BMS-903452 with a DPP-4 inhibitor synergistically augmented GLP-1 levels. BMS-903452 (0.03 mg/kg/day) also reduced fasting plasma glucose levels with increased insulin levels in db/db mice. BMS-903452 was safe and tolerable in normal healthy volunteers given a single dose ranging from 0.1 to 120mg, but did not alter plasma GLP-1 within the first 24 h of treatment.

Storage & Handling

• Storage: 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

GPR119

Compound Identifiers

PubChem CID

53477157