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CAS NO.69558-55-0
98%(500-1000)Kilogram98%(100-500)Metric Ton
thymopentin
CAS: 69558-55-0
Molecular Formula: C30H49N9O9
| Name | thymopentin |
| Synonyms | TP-5 Immunox Timunox Thyopentin THYMOPENTIN thymopentin Sintomodulina Thymopent njection thymopentin (TP-5) Thymopoietin 32-36 32-36-Thymopoietin Thymopoietin II-(32-36) ThyMopentin for Injection Thymopoietin pentapeptide L-Arg-L-Lys-L-Asp-L-Val-L-Tyr-OH Thymopoietin pentapeptide-Fluorescin-isothiocyanate N~5~-(diaminomethylidene)ornithyllysyl-alpha-aspartylvalyltyrosine N~5~-(diaminomethylidene)-L-ornithyl-L-lysyl-L-alpha-aspartyl-L-valyl-L-tyrosine |
| CAS | 69558-55-0 |
| EINECS | 811-641-8 |
| InChI | InChI=1/C30H49N9O9/c1-16(2)24(28(46)38-22(29(47)48)14-17-8-10-18(40)11-9-17)39-27(45)21(15-23(41)42)37-26(44)20(7-3-4-12-31)36-25(43)19(32)6-5-13-35-30(33)34/h8-11,16,19-22,24,40H,3-7,12-15,31-32H2,1-2H3,(H,36,43)(H,37,44)(H,38,46)(H,39,45)(H,41,42)(H,47,48)(H4,33,34,35)/t19-,20-,21-,22-,24-/m0/s1 |
| Molecular Formula | C30H49N9O9 |
| Molar Mass | 679.77 |
| Density | 1.44±0.1 g/cm3(Predicted) |
| Solubility | DMSO:100 mg/mL (147.1 mM); Water:100 mg/mL (147.1 mM); Insoluble in ethanol. |
| Appearance | Powder |
| Color | White |
| pKa | 3.07±0.10(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Refractive Index | 1.635 |
| MDL | MFCD00214200 |
| Physical and Chemical Properties | TP is a polypeptide extracted from calf thymus and two similar types were found: thymopoietin-I (TP-I) and thymopoietin-II(TP-II). TP-II is 49 peptide, consisting of 13 amino acids. The structural difference between TP-I and TP-II was that TP-II of the peptide chains were changed from Silk 1 and Su 43 to TP-I gan 1 and Group 43. The pentapeptide of Jing 32-casein 36 showed TP-II T cell differentiation activity in vitro and in vivo. 49 amino acids in 5 have physiological activity, has been artificial synthesis of spermidine peptide 5, namely thymopentin (timopentin), and for clinical use. In addition, the splenin isolated from the bovine spleen is similar to TP-II, so it is called TP-III. TP-II of the synthetic 5 peptides are temporarily referred to as thymus (TPe), and TP-III of the synthetic 5 peptides are temporarily referred to as spleen (SPe). TP-II and TPe act on neuromuscular transmission, inducing the differentiation of T cell precursor cells in vitro, while inhibiting the differentiation of B cells. TP-III and SPe can induce the differentiation of T and B cell precursor cells. Ubiquitin is composed of 74 amino acid residues, which can induce the differentiation of T cells and B cells. It is widely found in animal tissues (including thymus) and plants and fungi cells, associated with immune function. |
| Use | Non-inhibitory function enhancer for the treatment of primary or secondary immunodeficiency |
| Introduction | Thymopentin TP5, whose English name is Thymopentin, is a synthetic immunoregulatory pentapeptide, is a very important immune-promoting active peptide drugs, can significantly improve human immunity, help humans effectively resist a variety of diseases, at the same time for a variety of diseases have significant and exact curative effect, broad market prospects, with good economic and social benefits. |
| mechanism of action | thymopentin has the function of inducing and promoting the differentiation, maturation and activation of T lymphocytes and its subsets, regulate the proportion of T lymphocytes, so that CD4 /CD8 tends to be normal; Regulation and enhancement of human cellular immune function, can promote the maturation of T lymphocytes in peripheral blood after mitogen activation, increases the secretion of various lymphokines (e. G., Alpha, Gamma Interferon, interleukin 2 or interleukin 3) by T cells after activation of various antigens or mitogens, increases the level of lymphokine receptors on T cells. It also enhances the lymphocyte response through activation of T helper cells. In addition, it may affect the chemotaxis of NK precursor cells that become more cytotoxic upon exposure to interferon, contributing to their therapeutic effects. In addition, the thymus five peptide can enhance the ability of the human body to resist radiation. Therefore, it has the role of regulating and enhancing the body's cellular immune function. |
| physiological function | thymopentin has the same function of regulating the immune system as Thymosin, which can induce the differentiation of pre-T lymphocytes, mature, regulating the immune activity of mature T lymphocytes. For a variety of immune disorders, such as congenital thymus, thymectomy, senile thymic atrophy hypofunction, infection, tumor and autoimmune diseases due to the proportion of different T lymphocyte subsets and functional changes caused by low immune function, the drug has to make the immune response to normal regulation. |
| pharmacological action | thymopoietin is an endogenous polypeptide in thymus tissue, containing 49 amino acids, it can promote the differentiation of thymus and peripheral T cells, regulate the immune function and other biological activities. The thymopentin (TP5), which is composed of the 32 to 36 amino acids of the active center of thymopoietin, contains only five amino acid residues, but can effectively maintain the biological activity of thymopoietin. Since its launch in Italy under the trade name Timunox in 1985, TP5 has been used as an immunomodulator in clinical use including chronic hepatitis B, AIDS, and severe acute respiratory syndrome (SARS). Such as disease treatment and prevention. [Pharmacological effects] 1. Induce and promote T cell differentiation and maturation. Regulation of T lymphocyte subsets to make CD4/CD8 normal. 3. Enhanced macrophage phagocytosis. 4. Enhance red blood cell mediated immune function. 5. Increase the viability of natural killer (NK) cells. 6. Increase the production level of interleukin-2 (IL-2) and the expression level of its receptor. 7. Enhanced interferon-gamma production by peripheral blood mononuclear cells. 8. Enhance the activity of SOD in serum. |
| preparation method | TP-5 there are two main preparation methods: liquid phase synthesis method and solid phase synthesis method. 1. Liquid-phase synthesis of TP-5:(1) TP-5 was synthesized by a liquid-phase method combining Boc (tert-butoxycarbonyl) and Fmoc (9-fluorenylmethoxycarbonyl) strategies: the protected amino acids are HCl · H-Tyr(Bzl)-OBzl, Boc-Val-OH, Fmoc-Asp(OtBu)-OH, Fmoc-Lys(Boc)-OH and Fmoc-Arg(Pbf)-OH, the condensation reagent was BOP-HOBt, the condensation time was 2 h, the reaction solvent was chloroform, and the base neutralization reagent was N-methylmorpholine (NMM). Finally, the protective group removal system was carried out by using trifluoromethanesulfonic acid/trifluoroacetic acid (TFMSA/TFA)+ anisole, and the reaction was carried out at 0 ℃ for 2 h. (2) liquid phase synthesis of TP-5 by Boc amino group protection strategy and carbon chain step-by-step growth method: amino group was protected by Boc-HCl/dioxane system, DCC-HOBt condensation to obtain fully protected Boc-Arg(Tos)-Lys(Z)-Asp(OBz1)-Val-Tyr(Bz1)-OMe, after saponification, using TFA/TFMSA + anisole, anisole sulfide and O-methylphenol, reaction at room temperature for 1H, the side chain was removed to obtain white crystals, and the total yield was 30% after purification. (3) using the liquid phase minimum protection strategy to synthesize TP-5 step by step: Amino acid protection strategy: HC1 · Tyr-OMe, Boc-Val-OH, Boc-Asp(OBz1)-OH, Boc-Lys(2C1Z)-OH, Z-Arg-OH, DCC-HOBt condensation to form dipeptide, tripeptide and tetrapeptide, HBTU condensation to form a protective pentapeptide, and finally using Pd/C hydrogen to remove the side chain protection to obtain the target product. On the premise of no larger side reaction, the side chain functional group is not protected as much as possible, and the strong acid cleavage of HF can be avoided. The conditions are relatively mild and more suitable for industrialization. 2. The solid-phase synthesis of tp-5 is mainly composed of Boc/Bzl and Fmoc/OtBu two synthetic protection strategies. (1)Boc solid phase synthesis method: the main strategy of Boc synthesis method is to use the Boc which can be removed by TFA as the α-amino group, and the side chain protection is benzyl alcohol. Synthesis of a Boc-amino acid derivative covalently cross-linked to Merrifield or MBHA resin, removal of Boc with TFA, neutralization of the free amino terminus with triethylamine, followed by activation by DCC, coupling of the next amino acid, finally, the HF method or TFMSA method is used for deprotection. (2)Fmoc solid phase synthesis method: the fundamental difference between Fmoc method and Boc method lies in the use of alkali removable Fmoc as a protective group of α-amino group, the side chain is protected by tert-butoxy group which can be removed by TFA, etc., and the resin is 90% TFA-resectable p-alkoxybenzyl alcohol resin and 1%TFA-resectable dialkoxybenzyl alcohol resin, the final deprotection avoids strong acid treatment. The advantage of Fmoc as an amino protecting group is that it is stable to acids and is not affected by treatment with reagents such as TFA, Only mild alkali treatment is needed, and β 2 elimination reaction can be removed without neutralization with tertiary amine, and the Fmoc group has characteristic ultraviolet absorption, which is easy to detect and carry out, and brings convenience to automated synthesis. However, the price of Fmoc protected amino acids is expensive, and the synthesis cost is correspondingly higher. In TP-5 Fmoc solid-phase synthesis, using Wang resin, DMF as solvent, DIC-HOBt condensation, side chain protection strategy: Fmoc-Arg(Pbf)-OH, Fmoc-Lys(Boc)-OH, fmoc-Asp (OtBu)-OH, Fmoc-Val-OH and Fmoc-Tyr(tBu)-OH. |
| Use | 1. For chronic hepatitis B patients over 18 years of age. 2. Various primary or secondary T lymphocyte deficiency diseases. 3. Some autoimmune diseases (such as rheumatoid arthritis, systemic lupus erythematosus, etc.). 4. Various diseases with low cellular immune function. 5. Adjuvant therapy of tumor. (2016-04-25) It has the function of immune activation, promoting T cell differentiation, regulating neuromuscular conduction, and treating myasthenia gravis. Adverse reactions and contraindications: occasional skin itching, rash, periorbital edema, medication local pain, erythema damage, severe Leukopenia. enhancer of immune function, for the treatment of primary or secondary immunodeficiency |
Mol Download Chemical properties
CAS:
69558-55-0
MF:
C30H49N9O9
MW:
679.77
EINECS:
811-641-8
MDL No.:
MFCD00214200
Density
1.44±0.1 g/cm3(Predicted)
storage temp.
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
solubility
DMF: 30 mg/ml; DMSO: 25 mg/ml; Ethanol: 1 mg/ml; PBS (pH 7.2): 10 mg/ml
form
Powder
pka
3.07±0.10(Predicted)
color
White
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