SML0911
TAK-779
≥98% (HPLC)
동의어(들):
N,N-Dimethyl-N-[4-[[[2-(4-methylphenyl)-6,7-dihydro-5H-benzohepten-8-yl]carbonyl]amino]benzyl]tetrahydro-2H-pyran-4-aminium chloride, TAK-799, Takeda 779
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C33H39ClN2O2
CAS Number:
Molecular Weight:
531.13
UNSPSC 코드:
51111800
NACRES:
NA.77
추천 제품
Quality Level
분석
≥98% (HPLC)
양식
powder
색상
white to beige
solubility
H2O: 3 mg/mL, clear (warmed)
저장 온도
2-8°C
SMILES string
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 key
VDALIBWXVQVFGZ-UHFFFAOYSA-N
애플리케이션
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. 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.
생화학적/생리학적 작용
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. In mice, TTAK-779 protects the brain from focal cerebral ischemia.
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.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
가장 최신 버전 중 하나를 선택하세요:
Midhat H Abdulreda et al.
Proceedings of the National Academy of Sciences of the United States of America, 108(31), 12863-12868 (2011-07-20)
Intravital imaging emerged as an indispensible tool in biological research, and a variety of imaging techniques have been developed to noninvasively monitor tissues in vivo. However, most of the current techniques lack the resolution to study events at the single-cell
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.
Opass Putcharoen et al.
Journal of virology, 86(2), 1119-1128 (2011-11-18)
HIV CCR5 antagonists select for env gene mutations that enable virus entry via drug-bound coreceptor. To investigate the mechanisms responsible for viral adaptation to drug-bound coreceptor-mediated entry, we studied viral isolates from three participants who developed CCR5 antagonist resistance during
Shinya Takami et al.
Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism, 22(7), 780-784 (2002-07-27)
The effect of a nonpeptide CC chemokine receptor antagonist, TAK-779, on ischemic brain injury resulting from 1-hour middle cerebral artery occlusion followed by 48-hour reperfusion was examined in ddY mice. On intracerebroventricular injection of vehicle or TAK-779, infarct volume in
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