TC 14012
目录号 : GC17122
TC14012, a serum-stable derivative of T140, is a selective and peptidomimetic CXCR4 antagonist with an IC50 of 19.
Cas No.:368874-34-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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. |
|
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].
TC14012 是 T140 的血清稳定衍生物,是一种选择性的 CXCR4 拮抗剂,IC50 为 19.3 nM。TC14012 是有效的 CXCR7 激动剂,可将 β-arrestin2 募集到 CXCR7,EC50 为 350 nM。TC14012 具有抗 HIV 活性和抗癌活性[1-3]。
293FT细胞中,TC14012(10-10-10-5M ; 37℃; 90分钟)以剂量依赖的方式诱导CXCR7与β-抑制素偶联[4]。在TC14012处理的(0-30µM) HUVECs中,CXCR7的特异性激活显著促进了HUVECs管状形成[5]。用TC14012处理MSCs,可能促进成骨或软骨分化[6]。
TC14012(10 mg/kg; i.p. ;每6 天 4次)显著提高AMI小鼠心脏结构指标左室内径-舒张/收缩压、EFFS和左室容积-舒张/收缩压。TC14012可减少AMI模型小鼠的心梗死面积,增加血管密度。TC14012促进体内血管生成,升高VWF、VEGFR2、p-SRC、p-PLC-γ水平及p-P38/t-P38比值[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.
| Cas No. | 368874-34-4 | SDF | |
| 分子式 | C90H140N34O19S2 | 分子量 | 2066.43 |
| 溶解度 | Soluble in Water | 储存条件 | Store at -80°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。