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Grapiprant

Chemical Structure : Grapiprant

CAS No.: 415903-37-6

Grapiprant (CJ-023423;AAT-007)

Catalog No.: PC-45077Not For Human Use, Lab Use Only.

Grapiprant (CJ-023423, AAT-007) is a potent, selective EP4 receptor antagonist with Ki values of 13/20 nM against human and rat EP(4) receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Grapiprant (CJ-023423, AAT-007) is a potent, selective EP4 receptor antagonist with Ki values of 13/20 nM against human and rat EP(4) receptors.
Grapiprant (CJ-023423) is highly selective for the human EP(4) receptor over other human prostanoid receptor subtypes.
Grapiprant (CJ-023423) 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.
Oral administration of Grapiprant (CJ-023423) significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE(2) (ED(50) = 12.8 mg/kg).
Grapiprant (CJ-023423) is also effective in models of acute and chronic inflammatory pain.
CJ-023,423 significantly reduces mechanical hyperalgesia in the carrageenan model.
Grapiprant (CJ-023423) significantly reverses complete Freund's adjuvant-induced chronic inflammatory pain response.

Physicochemical Properties

M.Wt 491.6052
Formula C26H29N5O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzenesulfonamide, N-[[[2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenyl]ethyl]amino]carbonyl]-4-methyl-

References

1. Kazunari Nakao, et al. J Pharmacol Exp Ther. 2007 Aug;322(2):686-94.

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