Grapiprant (CJ-023423, AAT-007)

Chemical Structure : Grapiprant

CAS No.: 415903-37-6

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货号: 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.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥3280	In stock
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	491.6052
分子式	C26H29N5O3S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
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-

参考文献

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