推荐产品
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
H2O: 3 mg/mL, clear (warmed)
儲存溫度
2-8°C
SMILES 字串
Cl.[N+](C5CCOCC5)(Cc1ccc(cc1)\N=C(/[O-])\C2=Cc3c(ccc(c3)c4ccc(cc4)C)CCC2)(C)C
InChI
1S/C33H38N2O2.ClH/c1-24-7-11-27(12-8-24)28-14-13-26-5-4-6-29(22-30(26)21-28)33(36)34-31-15-9-25(10-16-31)23-35(2,3)32-17-19-37-20-18-32;/h7-16,21-22,32H,4-6,17-20,23H2,1-3H3;1H
InChI 密鑰
VDALIBWXVQVFGZ-UHFFFAOYSA-N
應用
TAK-779 has been used to inhibit CC chemokine ligand 5 (CCL5)– C-C chemokine receptor type 5 (CCR5) interaction in vitro in natural killer (NK) cytotoxicity assay.[1] It has also been used as a blocker of CCR5 to study its effects and to evaluate the opening of the Panx-1 channels on peripheral blood mononuclear cells (PBMCs) isolated from human immunodeficiency virus (HIV)-infected individuals.[2]
生化／生理作用
TAK-779 inhibits human immunodeficiency virus (HIV) entrance by blocking the C-C chemokine receptor type 5 (CCR5). It also impairs the formation of atherosclerotic lesions by preventing T-helper 1 cells from entering the plaque. TAK-779 possesses anti-immunogenic properties. In an arthritis model, it could prevent the inflow of CCR5- and chemokine (C-X-C motif) receptor 3 (CXCR3)-positive T cells into inflamed joints.[3] In mice, TTAK-779 protects the brain from focal cerebral ischemia.[4]
TAK-779 is a potent, dual antagonist at chemokine receptors C-C chemokine receptor type 2 (CCR2) and C-C chemokine receptor type 5 (CCR5) with IC50 = 1.4 nM at CCR5 and 2.3 nM at CCR2. Antagonists of both CCR2 and CCR5 such as TAK-779 have been investigated for treatment of viruses, rheumatoid arthritis, multiple sclerosis, and cancer. CCR5 is particularly targeted for anti-HIV therapy, since HIV entry into cells requires chemokine coreceptors CCR5 and C-X-C motif chemokine receptor 4 (CXCR4).
TAK-779 is a potent, dual antagonist at chemokine receptors CCR2 and CCR5.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Sam Bastani et al.
Transplantation, 88(8), 995-1001 (2009-10-27)
BACKGROUND.: Recruitment of recipient mononuclear cells to the donor heart is a central event in the development of cardiac allograft vasculopathy (CAV). The role of individual chemokine receptors in this process is incompletely defined. TAK-779 (N,N-dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzocyclohepten-8-yl]carbonyl]amino]benzyl]tetra-hydro-2H-pyran-4-aminium chloride) is a synthetic
Mercedes Armand-Ugón et al.
The Journal of antimicrobial chemotherapy, 65(3), 417-424 (2010-01-14)
Identification of CCR5 as an antiretroviral target led to the development of several CCR5 antagonists in clinical trials and the approval of maraviroc. Evaluating the mechanism of drug resistance to CCR5 agents may have implications in the clinical development of
Lavina Gharu et al.
Virus research, 158(1-2), 216-224 (2011-04-29)
The mechanism by which strictly CCR5 using HIV-1 clade C variants exacerbate disease progression in absence of coreceptor switch is not clearly known. We previously reported HIV-1 clade C envelopes (Env) obtained from late stage Indian patients with expanded coreceptor
Ulf Karlsson et al.
AIDS research and human retroviruses, 25(12), 1297-1305 (2009-12-17)
Through the use of chimeric CXCR4/CCR5 receptors we have previously shown that CCR5-tropic (R5) HIV-1 isolates acquire a more flexible receptor use over time, and that this links to a reduced viral susceptibility to inhibition by the CCR5 ligand RANTES.
Theresa L Chang et al.
Journal of acquired immune deficiency syndromes (1999), 53(3), 292-302 (2010-01-13)
Macrophages are major HIV target cells. They support both productive and latent HIV-1 infection. Susceptibility of primary macrophages to HIV depends on the anatomical location and activation state of the cells. We demonstrate that peritoneal macrophages (PMs) are abundant in
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