Grapiprant

SKU: orb1296072

Description

Grapiprant (AAT-007) is a selective EP4 prostaglandin receptor antagonist, exhibiting a Ki of 24 nM for the canine recombinant EP4 receptor. This compound is utilized in research to investigate EP4-mediated pathways in vitro and has been studied in vivo for its potential role in managing pain and inflammation associated with osteoarthritis.

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 415903-37-6
• MW: 491.61
• Purity: 99.84% (May vary between batches)
• Formula: C₂₆H₂₉N₅O₃S
• SMILES: CCc1nc2c(C)nc(C)cc2n1-c1ccc(CCNC(=O)NS(=O)(=O)c2ccc(C)cc2)cc1
• Target: Prostaglandin Receptor
• Solubility: DMSO:48 mg/mL (97.64 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (5.09 mM)

Bioactivity

• Target IC50:
  EP4 (dog):24 nM (Ki)|EP4:35 nM
• In Vivo:
  Grapiprant (0-50 mg/kg; p.o; every 24 hours; for 9 months; beagles) is safe for long-term oral administration in dogs .
• Animal Research:
  Animal Model: 36 beagles of both sexes (9-month-old). Dosage: 0 mg/kg, 1 mg/kg, 6 mg/kg, or 50 mg/kg. Administration: Oral administration; every 24 hours; for 9 months

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture,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

inhibit, EP4, Grapiprant, Inhibitor, CJ 023423, CJ023423, CJ-023423, AAT 007, AAT007, AAT-007, RQ00000007, RQ-00000007, RQ 00000007, Prostaglandin Receptor, ProstaglandinReceptor

Compound Identifiers

PubChem CID

11677589