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Taltirelin

Taltirelin Structure
CAS No.
103300-74-9
Chemical Name:
Taltirelin
Synonyms
TA 0910;Taltirelin;Taltireline;Ceredist, TA-0910;Taltirelin Acetate;TA-0910, taltirelin;Taltirelin (TA0910);Taltirelin USP/EP/BP;Mitragynine Impurity 2;Taltirelin interMediate
CBNumber:
CB31177191
Molecular Formula:
C17H23N7O5
Molecular Weight:
405.41
MOL File:
103300-74-9.mol
MSDS File:
SDS
Modify Date:
2024/7/2 8:55:04

Taltirelin 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

Taltirelin Chemical Properties,Uses,Production

Description

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.

Uses

Taltirelin is a thyrotropin-releasing hormone analog.

Biological Activity

Synthetic thyrotropin-releasing hormone (TRH) analog. Displays ~ 30-100-fold more potent CNS activity and ~ 50-fold weaker endocrine activity than TRH. Antinociceptive and neuroprotective.

Taltirelin Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 145)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
CLEARSYNTH LABS LTD. +91-22-45045900 Hyderabad, India 6351 58 Inquiry
Pharmaffiliates Analytics and Synthetics P. Ltd +91-172-5066494 Haryana, India 6773 58 Inquiry
Pharma Affiliates 172-5066494 Haryana, India 6761 58 Inquiry
Sigma Audley +86-18336680971 +86-18126314766 China 497 58 Inquiry
Capot Chemical Co.,Ltd. 571-85586718 +8613336195806 China 29798 60 Inquiry
Shenzhen Nexconn Pharmatechs Ltd +86-755-89396905 +86-15013857715 China 10318 58 Inquiry
Shaanxi Pioneer Biotech Co., Ltd . +8613259417953 China 3000 58 Inquiry
CONIER CHEM AND PHARMA LIMITED +8618523575427 China 49391 58 Inquiry
career henan chemical co +86-0371-86658258 +8613203830695 China 29826 58 Inquiry
Fuxin Pharmaceutical +86-021-021-50872116 +8613122107989 China 10297 58 Inquiry
Taltirelin interMediate (4S)-Hexahydro-1-Methyl-2,6-dioxo-4-pyriMidinecarbonyl-L-histidyl- Ceredist, TA-0910 TALTIRELIN INTERMEDIATES Taltirelin Acetate,TA-0910 Taltirelin L-Prolinamide, N-[(hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl)carbonyl]-L-histidyl-, (S)- L-Prolinamide, N-[[(4S)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-L-histidyl- (9CI) TA 0910 (4S)-N-[(2S)-1-[(2S)-2-Carbamoylpyrrolidin-1-yl]-3-(3H-imidazol-4-yl)-1-oxopropan-2-yl]-1-methyl-2,6-dioxo-1,3-diazinane-4-carboxamide 2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl- L-Prolinamide,(4S)-hexahydro-1-methyl- (6S)-N-[(S)-1-[[(2S)-2-Carbamoylpyrrolizino]carbonyl]-2-(1H-imidazole-4-yl)ethyl]-2,4-dioxo-3-methylhexahydropyrimidine-6-carboxamide 1-[Nα-[[(4S)-1-Methyl-2,6-dioxohexahydropyrimidine-4-yl]carbonyl]-L-histidyl]-L-prolinamide N-[[[(4S)-1-Methyl-2,6-dioxohexahydropyrimidin]-4α-yl]carbonyl]-L-His-L-Pro-NH2 Taltireline Taltirelin Acetate 1-METHYL-4,5-DIHYDROOROTYL-HIS-PRO-NH2 TA-0910, taltirelin N-[[(4S)-Hexahydro-1-methyl-2,6-dioxo-4-pyrimidinyl]carbonyl]-L-histidyl-L-prolinamide L-Prolinamide, (4S)-hexahydro-1-methyl-2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl- Taltirelin USP/EP/BP Taltirelin (TA0910) Taltirelin acetate salt Mitragynine Impurity 2 103300-74-9 C19H27N7O7 Neurochemicals Pharmaceuticals Peptide Chiral Reagents Heterocycles Intermediates & Fine Chemicals