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Grapiprant

Cat. No. M8971
Grapiprant Structure
Synonym:

CJ-023423; RQ-00000007; AAT-007

Size Price Availability
5mg USD 243  USD270 4-7 Days
10mg USD 423  USD470 4-7 Days
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro, Grapiprant 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. Grapiprant is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes. Grapiprant 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 Grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 491.61
Formula C26H29N5O3S
CAS Number 415903-37-6
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection.
Vito V, et al. J Pharm Biomed Anal. 2016 Jan 25;118:251-258. PMID: 26580822.

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.
Rausch-Derra LC, et al. Am J Vet Res. 2015 Oct;76(10):853-9. PMID: 26413822.

Effects of the selective EP4 antagonist, CJ-023,423 on chronic inflammation and bone destruction in rat adjuvant-induced arthritis.
Okumura T, et al. J Pharm Pharmacol. 2008 Jun;60(6):723-30. PMID: 18498708.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Grapiprant, CJ-023423; RQ-00000007; AAT-007 supplier, Prostaglandin Receptor, inhibitors

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