Thymopentin acetate
(Synonyms: 胸腺五肽醋酸盐) 目录号 : GC39199
A pentapeptide fragment of thymopoietin
Cas No.:89318-88-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Thymopentin is a pentapeptide fragment of thymopoietin.1 It induces prothymocyte differentiation in isolated mouse splenocytes when used at concentrations ranging from 0.018 to 18 ?M. Thymopentin (1 ?g/ml) increases proliferation of, and phytohemagglutinin-stimulated IL-2 production in, isolated human peripheral blood lymphocytes (PBLs).2 It reduces the number of splenic autologous rosette-forming cells in athymic mice when administered at doses ranging from 0.02 to 10 mg/kg.1 Adoptive cell transfer of splenocytes isolated from tumor-bearing mice administered thymopentin (100 ng/animal) reduces recipient tumor growth in a murine Lewis lung carcinoma model.3
1.Goldstein, G., Scheid, M.P., Boyse, E.A., et al.A synthetic pentapeptide with biological activity characteristic of the thymic hormone thymopoietinScience204(4399)1309-1310(1979) 2.Duchateau, J., Servais, G., Cooman, R., et al.In vitro influence of thymopentin on proliferative responses and phytohemagglutinin-induced interleukin 2 production in normal human lymphocyte culturesSurv. Immunol. Res.4(1)116-124(1985) 3.Lau, C.Y., Wang, E.Y., and Goldstein, G.Studies of thymopoietin pentapeptide (TP5) on experimental tumorsCell Immunol.66(2)217-232(1982)
| Cas No. | 89318-88-7 | SDF | |
| 别名 | 胸腺五肽醋酸盐 | ||
| 分子式 | C32H53N9O11 | 分子量 | 739.82 |
| 溶解度 | Soluble in DMSO | 储存条件 | -20°C, away from moisture and light |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.3517 mL | 6.7584 mL | 13.5168 mL |
| 5 mM | 0.2703 mL | 1.3517 mL | 2.7034 mL |
| 10 mM | 0.1352 mL | 0.6758 mL | 1.3517 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。
Exploring ex vivo peptideolysis of Thymopentin and lipid-based nanocarriers towards oral formulations
Int J Pharm 2022 Sep 25;625:122123.PMID:35995317DOI:10.1016/j.ijpharm.2022.122123.
The oral delivery of medicines is the most popular route of administration for patients. However, Thymopentin (TP5) is only available in the market in forms for parenteral administration. In large part, this is because of extensive peptidolytic degradation in the gastrointestinal tract (GIT), which decreases the amount of TP5 available for absorption. This study aims to understand the extent of TP5 peptideolysis and determine effective inhibitors and suitable lipid-based nanocarriers to aid in the development of an effective oral delivery formulation. Enzymatic degradation kinetics of TP5 was investigated in the presence or absence of mucosal and luminal components extracted from various parts of the rat intestine, including the duodenum, jejunum, ileum, and colon. Inhibition of TP5 enzymatic peptidolysis was screened in the presence or absence of EDTA, trypsin and chymotrypsin inhibitors from soybean (SBTCI), and bestatin. TP5 with SBTCI was loaded into lipid-based nanocarriers, including microemulsions, niosomes and solid lipid nanoparticles. These TP5-loaded nanocarriers were investigated through characterization of morphology, particle size, zeta potential, entrapment efficacy (EE%), and ex vivo rat intestinal degradation studies to select a lead formulation for a future oral drug delivery study. The degradation kinetics of TP5 followed pseudo-first-order kinetics, and the biological metabolism of TP5 was displayed in the presence of luminal contents, indicating that TP5 is sensitive to luminal enzymes. Notably, a considerable decrease in TP5 peptidolysis was found in the presence of SBTCI, bestatin, and EDTA. TP5 and SBTCI were loaded into three lipid-based delivery systems, displaying superior protection under ex vivo intestinal luminal contents and mucosal homogenates for 6 h compared with the pure drug solution. These findings suggest that using select inhibitors and lipid-based nanocarriers can decrease peptide degradation and may improve oral bioavailability of TP5 following oral administration.
Separation and purification of Thymopentin with molecular imprinting membrane by solid phase extraction disks
J Pharm Biomed Anal 2015 Jan;102:137-43.PMID:25265188DOI:10.1016/j.jpba.2014.07.016.
The synthesis and performance of molecularly imprinted membranes (MIMs) as a solid phase extraction packing materials for the separation and purification of Thymopentin from crude samples was described. In order to increase structural selectivity and imprinting efficiency, surface-initiated ATRP and ionic liquid (1-vinyl-3-ethyl acetate imidazolium chloride) were used to prepare molecularly imprinting membranes. The results demonstrated that solid phase extraction disks stuffed by MIMs with ionic liquids as functional monomer demonstrated high isolation and purification of performance to the Thymopentin. The molecular recognition of Thymopentin was analyzed by using molecular modeling software.
Trypsin-catalyzed kinetically controlled synthesis of a precursor dipeptide of Thymopentin in organic solvents, using a free amino acid as nucleophile
Prep Biochem Biotechnol 2004 Feb;34(1):45-56.PMID:15046296DOI:10.1081/PB-120027112.
Trypsin-catalyzed, kinetically controlled synthesis of a precursor, dipeptide of Thymopentin (TP-5), Bz-Arg-Lys-OH (or-OEt) in organic solvents was studied. Bz-Arg-OEt was used as the acyl donor and Lys-OH and Lys-OEt were used as the nucleophiles. Ethanol was selected as the organic solvent from ethanol, methanol, acetonitrile, and ethyl acetate tested under the experimental conditions. As expected, Lys-OEt is not a suitable nucleophile in trypsin-catalyzed reaction, due to its competition with the protective Arg-OEt as acyl donor for the active site of trypsin, while Lys-OH does not have this problem. The optimal reaction condition for the synthesis of Bz-Arg-Lys-OH was set up as 20% Tris-HCl buffer, pH 8.0, 35 degrees C for 6 h with the yield of 52.5%, or for 18-24 h with the yield of about 60%.
Peptide chiral purity determination: hydrolysis in deuterated acid, derivatization with Marfey's reagent and analysis using high-performance liquid chromatography-electrospray ionization-mass spectrometry
J Chromatogr A 1995 Jul 21;707(2):233-44.PMID:7633594DOI:10.1016/0021-9673(95)00352-n.
A high-performance liquid chromatography-electrospray ionization-mass spectrometric (LC-ESI-MS) method is presented that allows rapid and accurate determination of amino acid chiral purity in a peptide. Peptides are hydrolyzed in hydrochloric acid-d1/acetic acid-d4 and then converted to diastereomers by derivatization with 1-fluoro-2,4-dinitrophenyl-5-L-alanine amide (FDAA, Marfey's reagent). Mixtures of D- and L-amino acid diastereomeric pairs are resolved in one chromatographic separation using conventional reversed-phase high-performance liquid chromatography. Hydrolysis in a deuterated solvent is necessary because the original ratio of D-/L-amino acids present in a peptide changes during acid hydrolysis due to racemization. Peptide hydrolysis in deuterated acids circumvents this problem by labeling each amino acid that racemizes with one deuterium at the alpha-carbon. An increase in molecular mass of one atomic mass unit allows racemized amino acids to be distinguished from non-racemized amino acids by mass spectrometry. This procedure was used to determine the chiral purity of each amino acid in a purified, hexapeptide by-product (Arg-Lys-Lys-Asp-Val-Tyr) present in a kilogram batch of the synthetic pentapeptide, Thymopentin (Arg-Lys-Asp-Val-Tyr).
CD10 (endopeptidase 24.11) is a thymic peptide-degrading enzyme possibly involved in the regulation of thymocyte functions
Cell Immunol 1997 Jan 10;175(1):85-91.PMID:9015192DOI:10.1006/cimm.1996.1045.
Human immature thymocytes express significant levels of the CD10 (endopeptidase 24.11) cell surface antigen. We report here that IOB5, an anti-CD10 mAb, as well as the phorbol ester PMA down-regulate CD10 activity at the surface of human thymocytes. The kinetics of CD10 modulation were drastically different for both effectors, indicating different regulatory mechanisms. We also demonstrated that intact human thymocytes hydrolyze Thymopentin and that CD10 significantly participates in this process. Finally, we found that Thymopentin and to a lesser extent phosphoramidon, a specific endopeptidase 24.11 inhibitor, induced up-regulation of CD4 and CD8 molecules at the thymocyte cell surface. In view of these results, we suggest that down-regulation of endopeptidase 24.11 at the thymocyte cell surface might reduce its activity toward thymic factors possibly involved in the regulation of thymocyte functions.