327613-57-0
基本信息
AMD 15057
BIO-5192 (BIO5192)
(2(S)-[1-(3,5-Dichlorophenylsulfonyl)-L-prolylaMino]-4-[N-Methyl-N-[2-[4-[3-(2-Methylphenyl)ureido]phenyl]acetyl]-L-leucylaMino]butyric acid )
(S)-2-((S)-1-((3,5-dichlorophenyl)sulfonyl)pyrrolidine-2-carboxamido)-4-((S)-4-methyl-2-(N-methyl-2-(4-(3-(o-tolyl)ureido)phenyl)acetamido)pentanamido)butanoic acid
(2S)-2-[[[(2S)-1-[(3,5-Dichlorophenyl)sulfonyl]-2-pyrrolidinyl]carbonyl]amino]-4-[[(2S)-4-methyl-2-[methyl[2-[4-[[[(2-methylphenyl)amino]carbonyl]amino]phenyl]acetyl]amino]-1-oxopentyl]amino]butanoic acid
Butanoic acid, 2-[[[(2S)-1-[(3,5-dichlorophenyl)sulfonyl]-2-pyrrolidinyl]carbonyl]amino]-4-[[(2S)-4-methyl-2-[methyl[2-[4-[[[(2-methylphenyl)amino]carbonyl]amino]phenyl]acetyl]amino]-1-oxopentyl]amino]-, (2S)-
物理化学性质
| 熔点 | 134 - 136°C |
| 密度 | 1.380±0.06 g/cm3(Predicted) |
| 储存条件 | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| 溶解度 | 二甲基亚砜（微溶） |
| 酸度系数(pKa) | 3.52±0.10(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至灰白色 |
常见问题列表
|
α4β1 1.8 nM (IC 50 ) |
α9β1 138 nM (IC 50 ) |
α2β1 1053 nM (IC 50 ) |
α4β7 >500 nM (IC 50 ) |
The combination of BIO5192 (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization.
BIO5192 (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis).
BIO5192 (1 mg/kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 (3, 10, and 30 mg/kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 2.5-fold from 5,460 h*ng/ml for the 3 mg/kg dose to 14,175 h*ng/ml for the 30 mg/kg.
| Animal Model: | C57BL/6J x 129Sv/J F1 mice |
| Dosage: | 1 mg/kg (with Plerixafor: 5 mg/kg) |
| Administration: | I.v. |
| Result: | Exerted an additive effect on progenitor mobilization. |
| Animal Model: | Healthy female Lewis rats weighing 150g |
| Dosage: | 30 mg/kg |
| Administration: | S.c; bid; during days 5 through 14 |
| Result: | Showed a 3-day delay in onset of disease. |