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Grapiprant

品牌
Sigma-Aldrich
CAS
415903-37-6
货号
SML3183
规格纯度
≥98% (HPLC)
参考价格
1179.67 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

生化/生理作用

Grapiprant (CJ-023423) is an orally available, a potent and selective EP4 receptor antagonist that exhibits significant inhibitory effects on paw swelling, inflammatory biomarkers, synovial inflammation and bone destruction in AIA rats. Grapiprant is highly selective for the human EP4 receptor over other human prostanoid receptor subtypes. It also inhibits PGE2-evoked elevation in intracellular cAMP at the human and rat EP4 receptors with pA2 of 8.3 and 8.2 nM, respectively. In vivo, oral administration of grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE2 (ED50 = 12.8 mg/kg). It is also effective in models of acute and chronic inflammatory pain. Grapiprant significantly reduces mechanical hyperalgesia in the carrageenan model. Furthermore, it significantly reverses complete Freund′s adjuvant-induced chronic inflammatory pain response. It produces antihyperalgesic effects in animal models of inflammatory pain. Grapiprant is approved and widely used for treatment of osteoarthritis related pain in dogs. Grapiprant is classify as a non-cyclooxygenase inhibiting non-steroidal anti-inflammatory drug (NSAID).

基本信息

经验(实验)分子式C26H29N5O3S
分子量491.61
MDL编号MFCD16628076

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度2-8℃
SMILES stringO=C(NS(C1=CC=C(C)C=C1)(=O)=O)NCCC2=CC=C(N3C(CC)=NC4=C3C=C(C)N=C4C)C=C2

安全信息

象形图GHS07
警示用语:Warning
危险声明H302
预防措施声明P264 - P270 - P301 + P312 - P501
危险分类Acute Tox. 4 Oral
储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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