| 产品描述： | TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells. |
| 靶点： |
MIP-1α-CCR5:1 nM (IC50, in CHO/CCR5 cells);MIP-1β-CCR5:1 nM (IC50, in CHO/CCR5 cells);RANTES-CCR5:1.4 nM (IC50, in CHO/CCR5 cells);MCP-1-CCR2b:27 nM (IC50, in CHO/CCR5 cells);R5 HIV-1 (Ba-L):1.2 nM (EC50, in MAGI-CCR5 cells);R5 HIV-1 (Ba-L):5.7 nM (EC90, in MAGI-CCR5 cells);R5 HIV-1 (Ba-L):3.7 nM (EC50, in PBMCs);R5 HIV-1 (Ba-L):12.8 nM (EC90, in PBMCs);R5 HIV-1 (KK):1.6 nM (EC50, in PBMCs);R5 HIV-1 (KK):20.8 nM (EC90, in PBMCs);R5 HIV-1 (HHA):3.2 nM (EC50, in PBMCs);R5 HIV-1 (HHA):7.5 nM (EC90, in PBMCs);R |
| 体外研究： |
TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a Ki of 1.1 nM, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells. TAK-779 less potently blocks the binding of [125I]-monocyte chemotactic protein 1 to CCR2b in CHO/CCR2b cells, with an IC50 for CCR2b of 27 nM. TAK-779 also completely inhibits the binding of [125I]-RANTES to CHO/CCR5 cells with an IC50 of 1.4 nM. TAK-779 (20 nM) selectively inhibits CCR5-mediated Ca2+-signaling. In addition, TAK-779 shows no inhibition on X4 HIV-1 strains. TAK-779 is an antagonist of CXCR3, and inhibits the migration of T cells but not T cell proliferation |
| 体内研究： |
TAK-779 (10 mg/kg per day, s.c.) significantly prolongs the allograft survival of the rat intestinal transplantation model. TAK-779 also decreases the number of CD4+ as well as CD8+ T cells in spleen, blood and recipient mesenteric lymph nodes (MLN). TAK-779 (150 µg per mouse, s.c.) supppresses the development of experimental autoimmune encephalomyelitis (EAE) in myelin oligodendrocyte glycoprotein (MOG)-immunized C57BL/6 mice. TAK-779 decreases the infiltration of CXCR3 and CCR5 bearing leukocytes into the spinal cord. TAK-779 does not alter myelin oligodendrocyte glycoprotein (MOG)-specific immune responses or affect the potential of MOG-specific T cells to transfer experimental autoimmune encephalomyelitis (EAE) |
| 参考文献： |
1. Baba M, et al. A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci U S A. 1999 May 11;96(10):5698-703. 2. Takama Y, et al. Effects of a calcineurin inhibitor, FK506, and a CCR5/CXCR3 antagonist, TAK-779, in a rat small intestinal transplantation model. Transpl Immunol. 2011 Jul;25(1):49-55. 3. Ni J, et al. The chemokine receptor antagonist, TAK-779, decreased experimental autoimmune encephalomyelitis by reducing inflammatory cell migration into the central nervous system, without affecting T cell function. Br J Pharmacol. 2009 Dec;158(8):2046-5 4. Gao P, et al. The unique target specificity of a nonpeptide chemokine receptor antagonist: selective blockade of two Th1 chemokine receptors CCR5 and CXCR3. J Leukoc Biol. 2003 Feb;73(2):273-80. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.883 ml |
9.414 ml |
18.828 ml |
| 5 mM |
0.377 ml |
1.883 ml |
3.766 ml |
| 10 mM |
0.188 ml |
0.941 ml |
1.883 ml |
| 50 mM |
0.038 ml |
0.188 ml |
0.377 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京