Taltirelin , ≥98% , 103300-74-9
Synonym(s):
(4S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl-L-prolinamide;(S)-N-((S)-1-((S)-2-Carbamoylpyrrolidin-1-yl)-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxamide;(S)-N-[(Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl]-L-histidyl-L-prolinamide
| Pack Size | Price | Stock | Quantity |
| 5mg | RMB669.60 | In Stock |
|
| 10mg | RMB896.00 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 72-75° |
| alpha | 25D -13.6° (c = 1 in water) |
| Density | 1.447±0.06 g/cm3(Predicted) |
| storage temp. | Store at +4°C |
| form | Solid |
| pka | 9.32±0.40(Predicted) |
| color | White to off-white |
| Water Solubility | Soluble to 50 mM in sterile water |
| InChIKey | PGQRTQMGGUFKCM-DLOVCJGASA-N |
| SMILES | C(N)(=O)[C@@H]1CCCN1C(=O)[C@H](C[C@@H]1NCNC1)NC(C1=CC(=O)N(C)C(=O)N1)=O |
Description and Uses
Taltirelin was marketed in Japan for the treatment of neurodegenerative diseases, in particular the improvement of ataxia due to spino-cerebellar degeneration (SCD); it is the first orally-active drug in this indication. This synthetic thyrotropin-releasing hormone (TRH) analog is prepared by condensation of (S)-1-methyl-4,5-dihydroorotic acid with L-histidyl-Lprolinamide. It was shown that the S-configuration for all 3 chiral centers is crucial for CNS activity. Taltirelin is a potent agonist of the TRH receptors that shows significant effects on the cerebral monoamine systems when administered i.p. in rats. As TRH at 10-fold higher doses, taltirelin has been found to increase the extracellular levels of dopamine and its metabolites (DOPAC and HVA) as well as precursors and/or metabolites of noradrenaline and serotonin in different areas of the rat brain. Taltirelin produced an anti-ataxic activity in the Rolling mouse Nagoya, an ataxic mutant mouse. In several clinical studies performed in patients suffering from various forms of SCD, taltirelin demonstrated a statistically significant increase in the global improvement of ataxic symptoms and other neurologic abnormalities.
Taltirelin is a thyrotropin-releasing hormone analog.
