Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C33H54N12O15 |
Molecular Weight | 858.8533 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 7 / 7 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H](NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(O)=O
InChI
InChIKey=LIFNDDBLJFPEAN-BPSSIEEOSA-N
InChI=1S/C33H54N12O15/c1-15(39-29(55)18-6-8-24(50)40-18)27(53)42-16(4-2-3-9-34)30(56)45-21(14-47)32(58)43-17(5-7-22(35)48)28(54)38-11-25(51)37-12-26(52)41-20(13-46)31(57)44-19(33(59)60)10-23(36)49/h15-21,46-47H,2-14,34H2,1H3,(H2,35,48)(H2,36,49)(H,37,51)(H,38,54)(H,39,55)(H,40,50)(H,41,52)(H,42,53)(H,43,58)(H,44,57)(H,45,56)(H,59,60)/t15-,16-,17-,18-,19-,20-,21-/m0/s1
Nonathymulin (Thymulin, FTS) is well defined nonapeptide hormone produced by thymic epithelial cells. Its biological activity and antigenicity depend upon the presence of the metal zinc in the molecule. Thymulin consists of a biologically inactive nonapeptide component termed FTS (anacronym for serum thymus factor in French) coupled in an equimolecular ratio to the ion zinc, which confers biological activity to the molecule. This pharmacologically active metallopeptide induces the differentiation of T-cells and enhances several functions of the various T-cell subsets in normal or partially thymus-deficient recipients. The peptide is a natural hormone, available in synthetic form. Thymulin has a selective immunomodulatory effect, enhancing anti-inflammatory and inhibiting pro-inflammatory cytokines. It suppresses p38 (implicated in glucocorticoid-resistance) and inhibits NF-kappaB activation, which has an important pathogenic role in several lung diseases. The broad spectrum of anti-inflammatory effects of this peptide in several animal models of lung disease makes thymulin a good candidate for future clinical trials. Thymulin was being investigated by Santen Pharmaceutical in Japan. Its development for the treatment of ischaemic heart disorders and rheumatoid arthritis in Japan was discontinued. Thymulin is probably the best characterized of all putative thymic hormones and seems to playa physiological role in thymus–pituitary communication, particularly during perinatal life. Interest in the therapeutic use of thymulin flourished during the 1970s and 1980s when efforts were almost exclusively focused on using thymulin for the treatment of autoimmune and other immunopathologies as well as cancer. Subsequent studies established that thymulin is active on the hypophysis and the brain. This awareness and the availability of a synthetic gene for metFTS have opened new avenues for the exploration and eventual exploitation of the therapeutic potential of this metallopeptide.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/3310925
Two randomised double blind, placebo controlled trials have been carried out to assess the effectiveness of nonathymulin, a synthetic thymic peptide hormone, in the treatment of rheumatoid arthritis (RA) and to compare three different dosage schedules (1, 5, and 10 mg/day). Nonathymulin 5 mg proved to be the most efficient dose.
Route of Administration:
Other
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9719447
Effects of thymulin and thymulin augmentation of human chorionic gonadotropin (hCG) stimulation of testicular steroidogenesis were analyzed via incubation of testis from 3-, 6-, and 9-week-old rats with 0.1, 1, 10, and 100 ng/ml of thymulin or thymulin plus hCG (1 IU/ml). At three weeks of age, thymulin decreased testosterone and estrone synthesis. By 6 and 9 weeks of age, lower doses of thymulin (0.1 and 1 ng/ml) stimulated testosterone and estrone synthesis. Increased doses of thymulin (100 ng/ml) resulted in decreased testicular steroid synthesis.
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SUB09351MIG
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9H198D04WL
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CHEMBL2106455
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63958-90-7
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3085284
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9H198D04WL
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C174576
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DTXSID10213801
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THYMULIN
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5980
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100000083570
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ACTIVE MOIETY