SML3343
TC14012 Trifluoroacetate
≥95% (HPLC)
别名:
([Cit(6), D-Cit(8)]-T140 with C-terminal amide, TFA, H-Arg-Arg-Nal-Cys-Tyr-Cit-Lys-D-Cit-Pro-Tyr-Arg-Cit-Cys-Arg-NH2 (S–S bridged), TFA, R-R-Nal-C-Y-Cit-K-(D)Cit-P-Y-R-Cit-C-R-NH2 (S–S bridged), TFA, where Nal=L-3-(2-naphthylalanine)
生化/生理作用
CXCR4 antagonist and CXCR7 agonist that inhibits CXCR4-mediated HIV infection in cultures and ameliorates bleomycin-induced lung injury in vivo.
TC14012 is a highly stable and non-cytotoxic disulfide-bridged peptide with potent CXCR7 agonist and CXCR4 antagonist activity. TC14012 potently inhibits dual-tropic HIV strain 89.6 infection of CXCR4-expressing U87 glioblastoma cells (IC50 = 19.3 nM) and protects MT-4 cells against HIV-induced cytopathogenicity (EC50 = 0.4 nM). TC14012 also exhibits potent CXCR7-agonizing activity (HEK293T β-Arrestin recruitment EC50 = 350 nM; EC50 = 30 nM with CXCL12/SDF-1 and 140 μM with AMD3100). TC14012 (10 mg/kg i.t.) is efficacious in reducing repetitive bleomycin injections-induced collagen deposition and alveolar epithelial damage in a murine model of lung injury in vivo.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
此项目有
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Zhongwei Cao et al.
Nature medicine, 22(2), 154-162 (2016-01-19)
Although the lung can undergo self-repair after injury, fibrosis in chronically injured or diseased lungs can occur at the expense of regeneration. Here we study how a hematopoietic-vascular niche regulates alveolar repair and lung fibrosis. Using intratracheal injection of bleomycin
Nicolas Montpas et al.
Biochemistry, 54(7), 1505-1515 (2015-02-12)
The chemokine receptor CXCR7 is an atypical CXCL12 receptor that, as opposed to the classical CXCL12 receptor CXCR4, signals preferentially via the β-arrestin pathway and does not mediate chemotaxis. We previously reported that the cyclic peptide TC14012, a potent CXCR4
Toshina Oonuma et al.
The Journal of veterinary medical science, 65(10), 1069-1073 (2003-11-06)
It has recently been suggested that the chemokine receptor CXCR4 and its ligand SDF-1 (CXCL12) promote metastasis of various cancers in humans. Since feline mammary tumors also metastasize to distant organs frequently, we used real-time quantitative PCR to examine the
H Tamamura et al.
Bioorganic & medicinal chemistry letters, 11(14), 1897-1902 (2001-07-19)
We previously reported a truncated polyphemusin peptide analogue, T140, which efficiently inhibits infection of target cells by T-cell line-tropic strains of HIV-1 (X4-HIV-1) through its specific binding to a chemokine receptor, CXCR4. We have found that T140 is not stable
Stéphanie Gravel et al.
The Journal of biological chemistry, 285(49), 37939-37943 (2010-10-20)
CXCR7 is an atypical chemokine receptor that signals through β-arrestin in response to agonists without detectable activation of heterotrimeric G-proteins. Its cognate chemokine ligand CXCL12 also binds CXCR4, a chemokine receptor of considerable clinical interest. Here we report that TC14012
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