BIO5192 是一种选择性强的整合素 α4β1 (VLA-4) 抑制剂 (K_d<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。

BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (K d <10 pM). BIO5192 selectively binds to α4β1 (IC 50 =1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.

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α4β1 1.8 nM (IC50) α9β1 138 nM (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Ramirez P, et al. BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells. Blood. 2009;114(7):1340‐1343.
[2]. Leone DR, et al. An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis. J Pharmacol Exp Ther. 2003;305(3):

In Vitro: DMSO : 12.5 mg/mL (15.29 mM; ultrasonic and warming and heat to 60°C)配制储备液