Gosogliptin

SKU: orb1709562

Description

Gosogliptin is a potent, selective DPP-4 inhibitor that elevates active incretin levels (GLP-1, GIP) to enhance glucose-dependent insulin secretion. It is used in research for studying type 2 diabetes mechanisms and has demonstrated efficacy in both in vitro enzymatic assays and in vivo animal models.

Research Area

Protein Biochemistry

Key Properties

• CAS Number: 869490-23-3
• MW: 366.41
• Purity: 99.74% (May vary between batches)
• Formula: C₁₇H₂₄F₂N₆O
• SMILES: C(=O)([C@@H]1C[C@@H](CN1)N2CCN(CC2)C=3N=CC=CN3)N4CC(F)(F)CC4
• Target: DPP-4
• Solubility: DMSO:80 mg/mL (218.33 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (13.65 mM)

Bioactivity

• In Vivo:
  Methods: Gosogliptin (PF-00734200) was administered (orally) to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg) to investigate metabolism, pharmacokinetics, and excretion in Dawley (SD) rats, beagle dogs, and humans. Results: Gosogliptin recovered a mean of 97.1% of the administered radioactivity in urine, feces, and cage wash fluids within 168 hours after dosing. The mean cumulative dose recovered in feces was 66.0%. The mean cumulative excretion in urine was 30.8%. Approximately 95% of the excreted radioactivity was recovered within the first 48 hours.
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• In Vitro:
  Gosogliptin (PF-00734200) is a potent, oral, selective, and competitive DPP-IV inhibitor that rapidly and reversibly inhibits plasma DPP-4 activity when administered orally to rats, dogs, and monkeys.
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Storage & Handling

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

Alternative Names

Gosogliptin, DPP-IV, PF734200, PF-734200, PF 734200, PF00734200, PF-00734200, PF 00734200

Compound Identifiers

PubChem CID

11516136