BIO 5192
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- CAS号:
- 327613-57-0
- 英文名:
- (2(S)-[1-(3,5-Dichlorophenylsulfonyl)-L-prolylaMino]-4-[N-Methyl-N-[2-[4-[3-(2-Methylphenyl)ureido]phenyl]acetyl]-L-leucylaMino]butyric acid )
- 英文别名:
- BIO 5192;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)-
- 中文名:
- BIO 5192
- 中文别名:
- CBNumber:
- CB02641205
- 分子式:
- C38H46Cl2N6O8S
- 分子量:
- 817.78
- MOL File:
- 327613-57-0.mol
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BIO 5192化学性质
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熔点:
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134 - 136°C
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密度:
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1.380±0.06 g/cm3(Predicted)
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储存条件:
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Hygroscopic, -20°C Freezer, Under inert atmosphere
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溶解度:
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DMSO (Slightly)
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形态:
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Solid
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酸度系数(pKa):
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3.52±0.10(Predicted)
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颜色:
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White to Off-White
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BIO 5192性质、用途与生产工艺
BIO5192 是一种选择性强的整合素 α4β1 (VLA-4) 抑制剂 (Kd<10 pM)。BIO5192 选择性地与 α4β1 (IC50=1.8 nM) 结合,选择性高过其他一系列整合素。BIO5192 导致小鼠造血干细胞和祖细胞 (HSPCs) 的动员比基础水平增加 30 倍。
α4β1
1.8 nM (IC
50
)
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α9β1
138 nM (IC
50
)
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α2β1
1053 nM (IC
50
)
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α4β7
>500 nM (IC
50
)
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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:
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C57BL/6J x 129Sv/J F1 mice
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Dosage:
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1 mg/kg (with Plerixafor: 5 mg/kg)
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Administration:
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I.v.
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Result:
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Exerted an additive effect on progenitor mobilization.
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Animal Model:
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Healthy female Lewis rats weighing 150g
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Dosage:
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30 mg/kg
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Administration:
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S.c; bid; during days 5 through 14
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Result:
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Showed a 3-day delay in onset of disease.
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BIO 5192
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下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-107589 | BIO 5192 BIO5192 | 327613-57-0 | 5 mg | 2200元 |
2024/04/30 | HY-107589 | BIO 5192 BIO5192 | 327613-57-0 | 10 mg | 3500元 |
327613-57-0, BIO 5192 相关搜索:
- C38H46Cl2N6O8S
- 327613-57-0
- (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
- 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)-
- BIO-5192
(BIO5192)
- BIO 5192
- AMD 15057
- (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
- (2(S)-[1-(3,5-Dichlorophenylsulfonyl)-L-prolylaMino]-4-[N-Methyl-N-[2-[4-[3-(2-Methylphenyl)ureido]phenyl]acetyl]-L-leucylaMino]butyric acid )