TC 14012 |
| Katalog-Nr.GC17122 |
TC 14012, ein serumstabiles Derivat von T140, ist ein selektiver und peptidomimetischer CXCR4-Antagonist mit einem IC50 von 19,3 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 368874-34-4
Sample solution is provided at 25 µL, 10mM.
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TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.3 nM. TC14012 is a potent CXCR7 agonist with an EC50 of 350 nM for recruiting β-arrestin 2 to CXCR7. TC14012 has anti-HIV activity and anti-cancer activity [1-3].
TC14012(10-10-10-5M ; 37℃; 90 min) induce coupling of CXCR7 with β-arrestin in a dose-dependent manner in 293FT cell β-Arrestin recruitment assay[4]. In TC14012-treated(0-30µM) HUVECs(human umbilical vein endothelial cells), specific activation of CXCR7 significantly promoted the tubular formation of HUVECs[5]. TC14012 may promote osteogenesis or chondrodifferentiation in the treatment of mesenchymal stem cell (MSC) [6].
TC14012(10 mg/kg; i.p. ; 4 times every 6 days) significantly increased the left ventricular internal diameter-diastole/systole (LVID-d/s), a key cardiac structure index, and the EFFS, and left ventricular volume-diastole/systole (LV vol-d/s) in AMI mice. TC14012 reduced the infarct size and increased the vascular density in AMI model mice. TC14012 promoted angiogenesis in vivo, and TC14012 increased the levels of VWF, VEGFR2, p-SRC and p-PLC-γ as well as the p-P38/t-P38 ratio [7].
References:
[1]. Tamamura H, Omagari A, et,al. Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1897-902. doi: 10.1016/s0960-894x(01)00323-7. PMID: 11459656.
[2]. Gravel S, Malouf C, et,al. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem. 2010 Dec 3;285(49):37939-43. doi: 10.1074/jbc.C110.147470. Epub 2010 Oct 18. PMID: 20956518; PMCID: PMC2992227.
[3]. Gravel S, Malouf C, et,al. The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem. 2010 Dec 3;285(49):37939-43. doi: 10.1074/jbc.C110.147470. Epub 2010 Oct 18. PMID: 20956518; PMCID: PMC2992227.
[4]. Ishizuka M, Harada M, et,al. CXCR7 ameliorates myocardial infarction as a β-arrestin-biased receptor. Sci Rep. 2021 Feb 9;11(1):3426. doi: 10.1038/s41598-021-83022-5. Erratum in: Sci Rep. 2021 Jun 7;11(1):12340. PMID: 33564089; PMCID: PMC7873251.
[5]. Zhang M, Qiu L, et,al. CXCL12 enhances angiogenesis through CXCR7 activation in human umbilical vein endothelial cells. Sci Rep. 2017 Aug 15;7(1):8289. doi: 10.1038/s41598-017-08840-y. PMID: 28811579; PMCID: PMC5557870.
[6]. Wei ST, Huang YC, et,al. Gain of CXCR7 function with mesenchymal stem cell therapy ameliorates experimental arthritis via enhancing tissue regeneration and immunomodulation. Stem Cell Res Ther. 2021 May 29;12(1):314. doi: 10.1186/s13287-021-02402-w. PMID: 34051857; PMCID: PMC8164772.
[7]. Zhang S, Yue J, et,al. Activation of CXCR7 alleviates cardiac insufficiency after myocardial infarction by promoting angiogenesis and reducing apoptosis. Biomed Pharmacother. 2020 Jul;127:110168. doi: 10.1016/j.biopha.2020.110168. Epub 2020 Apr 28. PMID: 32361166.
| Cell experiment [1]: | |
|
Cell lines |
HEK293 transfected with human β-arrestin-2-ω and human CXCR7-α |
|
Preparation Method |
Cells were stimulated with human CXCL12 or TC14012 at 37℃ for 90 min and then, Gal-Screen was added and the cells were further incubated at 25℃ for 90 min. |
|
Reaction Conditions |
10-10-10-5M ; 37℃; 90 min |
|
Applications |
TC14012 induce coupling of CXCR7 with β-arrestin in a dose-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
C57BL/6 J mice (6-8 weeks old)( myocardial infarction model ) |
|
Preparation Method |
TC14012 (10 mg/kg) was dissolved in saline and intraperitoneally injected 4 times after coronary artery ligation every 6 days. |
|
Dosage form |
10 mg/kg; i.p. ;4 times every 6 days |
|
Applications |
TC14012 significantly increased the left ventricular internal diameter-diastole/systole (LVID-d/s), a key cardiac structure index, and ejection fraction (EF), fractional shortening (FS), and left ventricular volume-diastole/systole (LV vol-d/s) in Acute myocardial infarction (AMI) mice. |
|
References: [1]. Ishizuka M, Harada M, et,al. CXCR7 ameliorates myocardial infarction as a β-arrestin-biased receptor. Sci Rep. 2021 Feb 9;11(1):3426. doi: 10.1038/s41598-021-83022-5. Erratum in: Sci Rep. 2021 Jun 7;11(1):12340. PMID: 33564089; PMCID: PMC7873251. |
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| Cas No. | 368874-34-4 | SDF | |
| Formula | C90H140N34O19S2 | M.Wt | 2066.43 |
| Löslichkeit | DMSO : 25 mg/mL (12.10 mM; Need ultrasonic) | Storage | Store at -80°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 0.4839 mL | 2.4196 mL | 4.8393 mL |
| 5 mM | 0.0968 mL | 0.4839 mL | 0.9679 mL |
| 10 mM | 0.0484 mL | 0.242 mL | 0.4839 mL |
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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