Grapiprant

Grapiprant is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2).

Product information

CAS Number: 415903-37-6

Molecular Weight: 491.61

Formula: C26H29N5O3S

Synonym:

CJ-023423

RQ-00000007

AAT-007

Chemical Name: N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide

Smiles: CCC1=NC2=C(C=C(C)N=C2C)N1C1=CC=C(CCNC(=O)NS(=O)(=O)C2C=CC(C)=CC=2)C=C1

InChiKey: HZVLFTCYCLXTGV-UHFFFAOYSA-N

InChi: InChI=1S/C26H29N5O3S/c1-5-24-29-25-19(4)28-18(3)16-23(25)31(24)21-10-8-20(9-11-21)14-15-27-26(32)30-35(33,34)22-12-6-17(2)7-13-22/h6-13,16H,5,14-15H2,1-4H3,(H2,27,30,32)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 48 mg/mL (97.64 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

Grapiprant (0-50 mg/kg; p.o; every 24 hours; for 9 months; beagles) is safe for dogs by long-term oral administration [2].

References:

1. Vito VD, et al. Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection. J Pharm Biomed Anal. 2016 Jan 25;118:251-8.
2. Rausch-Derra LC, et al. Evaluation of the safety of long-term, daily oral administration of grapiprant, a novel drug for treatment of osteoarthritic pain and inflammation, in healthy dogs.Am J Vet Res. 2015 Oct;76(10):853-9.
3. Nagahisa A, et al. Pharmacology of grapiprant, a novel EP4 antagonist: receptor binding, efficacy in a rodent postoperative pain model, and a dose estimation for controlling pain in dogs. J Vet Pharmacol Ther. 2017 Jun;40(3):285-292.

Products are for research use only. Not for human use.