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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
BIO5192
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
327613-57-0
- 规格:
10mg/5mg
| 规格: | 10mg | 产品价格: | ¥3490.0 |
|---|---|---|---|
| 规格: | 5mg | 产品价格: | ¥2190.0 |
| 基本信息 | |
| CAS | No.327613-57-0 |
| 英文名称 | BIO5192 |
| 分子式 | C38H46Cl2N6O8S |
| 分子量 | 817.78 |
| 溶解性 | Soluble in DMSO(Need ultrasonic or Water bath) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:-20℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD26408178 |
| SMILES | CC1=CC=CC=C1NC(=O)NC2=CC=C(C=C2)CC(=O)N(C)C(CC(C)C)C(=O)NCCC(C(=O)O)NC(=O)C3CCCN3S(=O)(=O)C4=CC(=CC(=C4)Cl)Cl |
| InChIKey | MNQBPRHHZPXCKZ-ZDCRTTOTSA-N |
| InChI | InChI=1S/C38H46Cl2N6O8S/c1-23(2)18-33(45(4)34(47)19-25-11-13-28(14-12-25)42-38(52)44-30-9-6-5-8-24(30)3)35(48)41-16-15-31(37(50)51)43-36(49)32-10-7-17-46(32)55(53,54)29-21-26(39)20-27(40)22-29/h5-6,8-9,11-14,20-23,31-33H,7,10,15-19H2,1-4H3,(H,41,48)(H,43,49)(H,50,51)(H2,42,44,52)/t31-,32-,33-/m0/s1 |
| PubChem CID | 10350459 |
| 靶点 | Integrin(VLA-4) |
| 通路 | Cytoskeleton |
| 背景说明 | 是一种选择性强的整合素 α4β1 (VLA-4) 抑制剂 。 |
| 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[1][2]. |
| 细胞实验 | The combination of BIO5192 (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 (30 mg/kg; s.c; bid; during days 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2].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[1].Animal Model: C57BL/6J x 129Sv/J F1 mice[1];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[2];Dosage:30 mg/kg;Administration:S.c; bid; during days 5 through 14;Result:Showed a 3-day delay in onset of disease. |
| 数据来源文献 | [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): |
| 单位 | 瓶 |
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