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CJ-42794 (CJ-042794)是前列腺素受体 EP4的选择性拮抗剂, 抑制[3H]-PGE2与 EP4受体结合的平均 pKi 为8.5, 对 EP4选择性比 EP1, EP2和 EP3高200多倍。
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CJ-42794 (CJ-042794)是前列腺素受体 EP4的选择性拮抗剂, 抑制[3H]-PGE2与 EP4受体结合的平均 pKi 为8.5, 对 EP4选择性比 EP1, EP2和 EP3高200多倍。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 139 | 现货 | |
5 mg | ¥ 298 | 现货 | |
10 mg | ¥ 493 | 现货 | |
25 mg | ¥ 956 | 现货 | |
50 mg | ¥ 1,730 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 447 | 现货 |
产品描述 | CJ-42794 (CJ-042794) is a selective antagonist of prostaglandin E receptor subtype 4 (EP4). It inhibits [3H]-PGE2 binding to the human EP4 receptor (a mean pKi: 8.5). CJ-42794 is a binding affinity that was at least 200-fold more selective for the human EP4 receptor than other human EP receptor subtypes (EP1, EP2, and EP3) (IC50 : 8.5 (pKi )). |
体外活性 | CJ-042794 competitively inhibits PGE2-evoked elevations of intracellular cAMP levels in HEK293 cells overexpressing human EP4receptor (mean pA2: 8.6). CJ-042794 reverses the inhibitory effects of PGE2 on LPS-induced TNFα production in a concentration-dependent manner [1]. |
体内活性 | CJ-42794 significantly delays ulcer healing in rats and mice and these responses were both attenuated by coadministration of CJ-42794 [2]. |
别名 | CJ-042794 |
分子量 | 413.83 |
分子式 | C22H17ClFNO4 |
CAS No. | 847728-01-2 |
Smiles | C[C@H](NC(=O)c1cc(Cl)ccc1Oc1ccc(F)cc1)c1ccc(cc1)C(O)=O |
密度 | 1.347 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 28 mg/mL (67.66 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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