BIO 5192

生物活性靶点体内研究 BIO 5192 试剂级价格

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

BIO 5192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 :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。

靶点

α4β1

1.8 nM (IC ₅₀ )

α9β1

138 nM (IC ₅₀ )

α2β1

1053 nM (IC ₅₀ )

α4β7

>500 nM (IC ₅₀ )

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.