BIO 5192
- 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 )
- 中文名:BIO 5192
- CBNumber:CB02641205
- 分子式:C38H46Cl2N6O8S
- 分子量:817.78
- MOL File:327613-57-0.mol
- 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 :DMSO (Slightly)
- 形态 :Solid
- 酸度系数(pKa) :3.52±0.10(Predicted)
- 颜色 :White to Off-White
BIO 5192性质、用途与生产工艺
- 生物活性 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。
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靶点
α4β1
1.8 nM (IC 50 )
α9β1
138 nM (IC 50 )
α2β1
1053 nM (IC 50 )
α4β7
>500 nM (IC 50 )
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体内研究
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.
- 更新日期：2024/11/08
- 产品编号：HY-107589
- 产品名称：BIO 5192 BIO5192
- CAS编号：327613-57-0
- 包装：5 mg
- 价格：2200元
- 更新日期：2024/11/08
- 产品编号：HY-107589
- 产品名称：BIO 5192 BIO5192
- CAS编号：327613-57-0
- 包装：10 mg
- 价格：3500元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
