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Grapiprant (415903-37-6)

Grapiprant, also known as AT-001 and CJ-023, is a drug from the piprant class. These molecules were derived from acylsulfonamide and are characterized to be a novel series of para-N-acylaminomethylbenzoic acid known to be prostaglandin receptor antagonists.

Not Intended for Therapeutic Use. For research use only.

CAS: 415903-37-6 Category

Grapiprant (415903-37-6) Description:

Grapiprant, also known as CJ-023,423, RQ-00000007 and AAT-007, is a novel, potent and selective prostaglandin EP4 receptor antagonist with antihyperalgesic properties. It is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis.

In vitro, CJ-023,423 inhibits [(3)H]PGE(2) binding to both human and rat EP(4) receptors with K(i) of 13 +/- 4 and 20 +/- 1 nM, respectively. CJ-023,423 is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. It also inhibits PGE(2)-evoked elevation in intracellular cAMP at the human and rat EP(4) receptors with pA(2) of 8.3 +/- 0.03 and 8.2 +/- 0.2 nM, respectively. In vivo, oral administration of CJ-023,423 significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).

Grapiprant (415903-37-6) Specifications:

Product Name Grapiprant
Synonyms CJ-023423;CJ023423;AAT-007;AAT007;AAT 007; RQ-00000007; RQ 00000007; RQ00000007;
Chemical Name N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide;1-(2-(4-(2-ethyl-4,6-dimethylimidazo(4,5-c)pyridin-1-yl)phenyl)ethyl)-3-(4-methylphenyl)sulfonylurea
Purity ≥98%
CAS Number 415903-37-6
Molecular Formula C26H29N5O3S
Molecular Weight 491.60516
Monoisotopic Mass 491.199 g/mol
MDL number N/A
InChIKey HZVLFTCYCLXTGV-UHFFFAOYSA-N
InChi Code 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)
SMILES O=C(NCCC1=CC=C(C=C1)N2C(CC)=NC3=C(N=C(C=C32)C)C)NS(C4=CC=C(C=C4)C)(=O)=O
Form Powder
Color N/A
Solubility  Soluble in DMSO, not in water
Storage Temp.  -20°C
Shelf life ≥ 2 years
Handling Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Provide appropriate exhaust ventilation at places where dust is formed
Application It is currently under development for use in humans and dogs for the control of pain and inflammation associated with osteoarthritis.

 


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RIDADR NONH for all modes of transport

References:

  • Vito VD, Saba A, Lee HK, Owen H, Poapolathep A, Giorgi M. 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. doi: 10.1016/j.jpba.2015.11.004. Epub 2015 Nov 7. PubMed PMID: 26580822.
  • Rausch-Derra L, Huebner M, Wofford J, Rhodes L. A Prospective, Randomized, Masked, Placebo-Controlled Multisite Clinical Study of Grapiprant, an EP4 Prostaglandin Receptor Antagonist (PRA), in Dogs with Osteoarthritis. J Vet Intern Med. 2016 May;30(3):756-63. doi: 10.1111/jvim.13948. Epub 2016 Apr 13. PMID: 27075237 PMCID: PMC4913586.
  • De Vito V, Salvadori M, Poapolathep A, Owen H, Rychshanova R5, Giorgi M6. Pharmacokinetic/pharmacodynamic evaluation of grapiprant in a carrageenan-induced inflammatory pain model in the rabbit. J Vet Pharmacol Ther. 2017 Oct;40(5):468-475. doi: 10.1111/jvp.12380. Epub 2016 Dec 7. PMID: 27925221.
  • Rausch-Derra LC, Rhodes L. Safety and toxicokinetic profiles associated with daily oral administration of grapiprant, a selective antagonist of the prostaglandin E2 EP4 receptor, to cats. Am J Vet Res. 2016 Jul;77(7):688-92. doi: 10.2460/ajvr.77.7.688. PMID: 27347820.
  • Łebkowska-Wieruszewska B, Barsotti G, Lisowski A, Gazzano A, Owen H, Giorgi M. Pharmacokinetics and estimated bioavailability of grapiprant, a novel selective prostaglandin E2 receptor antagonist, after oral administration in fasted and fed dogs. N Z Vet J. 2017 Jan;65(1):19-23. Epub 2016 Oct 19. PMID: 27691904.

1 review for Grapiprant (415903-37-6)

  1. Cofttek

    Never had such good experience before,The Grapiprant (415903-37-6) is high purity,also customer service is pretty nice !gotta try!!

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