TAK-779

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TAK-779 是一种有效的、特异性的非肽 CCR5 拮抗剂，Kd 为 0.45 nM。

TAK-779 is a potent, specific, nonpeptide CCR5 antagonist with Kd of 0.45 nM, antagonizes CCR2b to a lesser extent (27 nM) but does not affect CCR1, CCR3, or CCR4; also blocks the binding of macrophage inflammatory protein 1α and macrophage inflammatory protein 1β to the cells with an IC50 of 1.0 nM; TAK-779 displays highly potent and selective inhibition of the replication of macrophage (M)-tropic HIV-1 (Ba-L strain) in both MAGI-CCR5 cells and PBMCs with EC50 of 1.2 and 3.7 nM, respectively.HIV Infection Discontinued.

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.

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).

TAK779 | TAK 799 | Takeda 779

Microbiology/Virology

HIV

HIV

Infection

HIV Infection

229005-80-5

531.1

C33H39ClN2O2

>98% (HPLC)

DMSO: ≥ 27 mg/mL

CC1=CC=C(C=C1)C2=CC3=C(CCCC(=C3)C(=O)NC4=CC=C(C=C4)C[N+](C)(C)C5CCOCC5)C=C2.[Cl-]

2H-Pyran-4-aminium, N-[[4-[[[6,7-dihydro-2-(4-methylphenyl)-5H-benzocyclohepten-8-yl]carbonyl]amino]phenyl]methyl]tetrahydro-N,N-dimethyl-, chloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years