SML3343
TC14012 Trifluoroacetate
≥95% (HPLC)
Synonym(s):
([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)
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About This Item
NACRES:
NA.77
UNSPSC Code:
51111800
Biochem/physiol Actions
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.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Wanshu Ma et al.
The Journal of biological chemistry, 288(22), 15481-15494 (2013-04-20)
The discovery of CXCR7 as a new receptor for SDF-1 places many previously described SDF-1 functions attributed to CXCR4 in question, though whether CXCR7 acts as a signaling or "decoy" receptor has been in debate. It is known that CXCR7
Meike Burger et al.
Blood, 106(5), 1824-1830 (2005-05-21)
Growth and survival of chronic lymphocytic leukemia (CLL) B cells are favored by interactions between CLL and nontumoral accessory cells. CLL cells express CXCR4 chemokine receptors that direct leukemia cell chemotaxis. Marrow stromal cells or nurselike cells constitutively secrete CXCL12
Wanshu Ma et al.
Biochemical pharmacology, 89(1), 99-108 (2014-03-04)
We have recently reported that CXCR7, the alternate high affinity SDF-1 receptor, is induced during monocyte-to-macrophage differentiation, leading to increased macrophage phagocytosis linked to atherosclerosis. Statins, the most widely used medications for atherosclerosis, were shown to have pleiotropic beneficial effects
Minqian Shen et al.
Ophthalmic research, 52(1), 17-24 (2014-05-24)
To observe the effect of TC14012 (a CXCR4 antagonist and CXCR7 agonist) on alkali burn-induced corneal neovascularization (CNV) in a mouse model. CNV was induced in vivo by alkali burns on the corneas of BALB/c mice. A total of 54
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
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