Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 신윤용 | * |
dc.contributor.author | 이화정 | * |
dc.contributor.author | 김대기 | * |
dc.date.accessioned | 2017-01-05T02:01:01Z | - |
dc.date.available | 2017-01-05T02:01:01Z | - |
dc.date.issued | 2008 | * |
dc.identifier.issn | 0049-8254 | * |
dc.identifier.other | OAK-4667 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/233567 | - |
dc.description.abstract | The authors investigated the pharmacokinetics and metabolism of 3-((5-(6-methylpyridin-2-yl)-4-(quinoxalin-6-yl)-1H-imidazol-2-yl)methyl) benzamide (IN-1130), a novel ALK5 inhibitor, which suppresses renal and hepatic fibrosis, and also exerts anti-metastatic effects on breast cancer-bearing MMTV-cNeu mice model. Plasma half-lives of orally administered IN-1130 were 62.6 min in mice, 76.6 ± 10.6 min in dogs, 156.1 ± 19.3 min in rats, and 159.9 ± 59.9 min in monkeys. IN-1130 showed a high apparent permeability coefficient (Papp) of (45.0 ± 2.3) × 10-6 cm s-1 in in vitro permeability tests in a Caco-2 cell monolayer model. The bioavailability of orally administered IN-1130 was 84.9% in dogs and 34.4% in monkeys (oral dose, 5.5 mg kg-1), 11.4% in rats and 8.95% in mice (oral dose, 50.3 mg kg-1), respectively. Orally given IN-1130 was readily distributed into liver, kidneys and lungs. The major metabolite of IN-1130 (M1) was detected in the systemic circulation of rat and mouse and was purified and tentatively identified as 3-((4-(3-hydroxyquinoxaline-6-yl)-5-(6-methylpyridine-2-yl)-1H-imidazol-2-yl) methyl)benzamide or 3-((4-(2-hydroxyquinoxalin-6-yl)-5-(6-methylpyridine-2-yl)- 1H-imidazol-2-yl)methyl)benzamide. The highest levels of M1 were found in liver. The results of this study suggest that IN-1130 has the potential to serve as an effective oral anti-fibrotic drug. © 2008 Informa UK Ltd. | * |
dc.language | English | * |
dc.title | Pharmacokinetics and tissue distribution of 3-((5-(6-methylpyridin-2-yl)-4- (quinoxalin-6-yl)-1H-imidazol-2-yl)methyl)benzamide; a novel ALK5 inhibitor and a potential anti-fibrosis drug | * |
dc.type | Article | * |
dc.relation.issue | 3 | * |
dc.relation.volume | 38 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 325 | * |
dc.relation.lastpage | 339 | * |
dc.relation.journaltitle | Xenobiotica | * |
dc.identifier.doi | 10.1080/00498250701781924 | * |
dc.identifier.wosid | WOS:000253905900007 | * |
dc.identifier.scopusid | 2-s2.0-39349112853 | * |
dc.author.google | Kim Y.W. | * |
dc.author.google | Kim Y.K. | * |
dc.author.google | Lee J.Y. | * |
dc.author.google | Chang K.T. | * |
dc.author.google | Lee H.J. | * |
dc.author.google | Kim D.-K. | * |
dc.author.google | Sheen Y.Y. | * |
dc.contributor.scopusid | 신윤용(6603872711) | * |
dc.contributor.scopusid | 이화정(57102029300) | * |
dc.contributor.scopusid | 김대기(35083694200) | * |
dc.date.modifydate | 20240118154655 | * |