SML3183

Grapiprant

≥98% (HPLC)

• 别名: 2-Ethyl-4,6-dimethyl-1-[4-[2-[[[[(4-methylphenyl)sulfonyl]amino]carbonyl]amino]ethyl]phenyl]-1H-imidazo[4,5-c]pyridine, CJ-023,423, CJ-023423, N-[({2-[4-(2-ethyl-4,6-dimethyl-1H-imidazo [4,5-c]pyridin-1-yl)phenyl]ethyl}amino)carbonyl]-4-methylbenzenesulfonamide
• 经验公式（希尔记法）: C₂₆H₂₉N₅O₃S
• CAS号: 415903-37-6
• 分子量: 491.61
• MDL號碼: MFCD16628076
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: white to beige
• 溶解度: DMSO: 2 mg/mL, clear
• 儲存溫度: 2-8°C
• SMILES 字串: O=C(NS(C1=CC=C(C)C=C1)(=O)=O)NCCC2=CC=C(N3C(CC)=NC4=C3C=C(C)N=C4C)C=C2

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).

安全信息

• 象形圖: GHS07
• 訊號詞: Warning
• 危險聲明: H302
• 防範說明: P264 - P270 - P301 + P312 - P501
• 危險分類: Acute Tox. 4 Oral
• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable