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TAK-779

CAS No. : 229005-80-5

MCE 国际站：TAK-779

产品活性：TAK-779 是一种有效的，选择性的，非肽类 CCR5 和 CXCR3 拮抗剂，对 CCR5 的 K_i 值为 1.1 nM，同时可以有效地，选择性地抑制 R5 HIV-1，在 MAGI-CCR5 细胞中，EC₅₀ 和 EC₉₀ 值分别为 1.2 nM 和 5.7 nM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation  |  Anti-infection

作用靶点：CCR  |  HIV  |  CXCR

In Vitro: TAK-779 is a potent and selective nonpeptide antagonist of CCR5, with a K_i 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.

In Vivo: 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).

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