中文名 | Porcupine-IN-1 |
英文名 | Porcupine-IN-1 |
别名 | 化合物PORCUPINE-IN-1 N-((3-氟-2'-甲基-[2,4'-联吡啶]-5-基)甲基)-9H-咔唑-2-甲酰胺 |
英文别名 | CS-2802 PORCN-IN-1 Porcupine-IN-1 Porcn inhibitor 1 Porcupine-IN-1 free base 9H-Carbazole-2-carboxamide, N-[(3-fluoro-2'-methyl[2,4'-bipyridin]-5-yl)methyl]- |
CAS | 2036044-77-4 |
化学式 | C25H19FN4O |
分子量 | 410.44 |
存储条件 | 2-8℃ |
MDL号 | MFCD31630804 |
体外研究 | Porcupine is an enzyme that catalyses the addition of palmitoleate to a serine residue in Wnt proteins, a process which is required for the secretion of Wnt proteins. Porcupine-IN-1 is as potent as the clinical compound LGK974 in a cell based STF reporter gene assay. Porcn-IN-1 potently inhibits the secretion of Wnt3A, therefore is confirmed to be a porcupine inhibitor. |
体内研究 | Porcn-IN-1 demonstrates moderate clearance under the treatment of human liver microsomes (57 mL/min/kg) and rat liver microsomes (24 mL/min/kg). It exhibits high clearance when treated with mouse microsomes (109 mL/min/kg). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.436 ml | 12.182 ml | 24.364 ml |
5 mM | 0.487 ml | 2.436 ml | 4.873 ml |
10 mM | 0.244 ml | 1.218 ml | 2.436 ml |
5 mM | 0.049 ml | 0.244 ml | 0.487 ml |
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