产品
编 号:F320873
分子式:C38H46Cl2N6O8S
分子量:817.78
产品类型
结构图
CAS No: 327613-57-0
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产品详情
生物活性:
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=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.
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.