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Grapiprant

Cat. No. M8971
Grapiprant Structure
Synonym:

CJ-023423; RQ-00000007; AAT-007

Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 150  USD150 In stock
25mg USD 250  USD250 In stock
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Quality Control & Documentation
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).

Chemical Information
Molecular Weight 491.61
Formula C26H29N5O3S
CAS Number 415903-37-6
Solubility (25°C) DMSO 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Vito V, et al. J Pharm Biomed Anal. Detection and quantification of the selective EP4 receptor antagonist CJ-023423 (grapiprant) in canine plasma by HPLC with spectrofluorimetric detection.

[2] Rausch-Derra LC, et al. Am J Vet Res. 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.

[3] Okumura T, et al. J Pharm Pharmacol. Effects of the selective EP4 antagonist, CJ-023,423 on chronic inflammation and bone destruction in rat adjuvant-induced arthritis.

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


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