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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

MDL Number:: MFCD00894697

MOL File:: 103300-74-9.mol

MSDS File:: SDS

Last updated:2024-01-17 18:41:23

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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
pka	9.32±0.40(Predicted)
Water Solubility	Soluble to 50 mM in sterile water
FDA UNII	DOZ62MV6A5

Taltirelin price More Price(14)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Tocris	2672	Taltirelin ≥96%(HPLC)	103300-74-9	1	$123	2021-12-16	Buy
TRC	T565305	Taltirelin	103300-74-9	5mg	$45	2021-12-16	Buy
Usbiological	289920	Taltirelin	103300-74-9	5mg	$418	2021-12-16	Buy
Usbiological	256806	Taltirelin	103300-74-9	1mg	$360	2021-12-16	Buy
Biosynth Carbosynth	FT27992	Taltirelin	103300-74-9	50mg	$400	2021-12-16	Buy

Product number	Packaging	Price	Buy
2672	1	$123	Buy
T565305	5mg	$45	Buy
289920	5mg	$418	Buy
256806	1mg	$360	Buy
FT27992	50mg	$400	Buy

Taltirelin Chemical Properties,Uses,Production

Oral thyrotropin-releasing hormone

Taltirelin is a pituitary hormone release stimulant,it is successfully developed by the Japanese Mitsubishi Tanabe Seiyaku Co. Ltd. ,its trade name is Taltirelin, it belongs to 3.1 class of new drugs of chemical drugs , currently it is used in clinical for improvement in patients with spinocerebellar degeneration,it is the most effective movement disorders drug.
Taltirelin is the world's first approved oral thyrotropin releasing hormone (TRH), in addition to having endocrine effects, it can also have effect on certain central nervous system (CNS) , including increasing locomotor activity, antagonistic reserpine-induced hypothermia, and antagonism of pentobarbital-induced sleep. The specie is developed by the Japanese Mitsubishi Tanabe Pharma Corporation in September 2000 for the first time in Japan, it is used to improve the ataxia in the patient's with spinocerebellar degeneration . Spinocerebellar ataxias (SCAs) formerly known as autosomal dominant ataxia, are a group of chronic degenerative diseases of the central nervous system with ataxia, dysmetria as the main clinical manifestations. In September 2000, thyrotropin releasing hormone (TRH)injection is the only drug for the treatment of such diseases. Taltirelin is the structural modification transform drug of TRH , pharmacological studies show that the product has strong and lasting multiple effects on CNS through brain TRH receptors . The excitatory effect of the product on CNS is 10 to 100 times stronger than TRH , the duration of action is about 8 times longer than TRH. The receptor affinity of the product is about 1/11 of TRH , and thus the endocrine effect of this product is weaker than TRH, but this product is more stable in vivo than TRH. In addition, the thyrotropin (TSH) release effect of the product is 1/6-1/11 of TRH , TSH release is regulated by a strong negative feedback system including thyroid hormone , it has a strong effect on the central nervous system, but while its hormone-like effect is small, and therefore it has fewer side effects. The main side effects are digestive reactions include vomiting, nausea and stomach discomfort. All adverse events are mild to moderate, they disappear during and (or) after treatment.
The above information is edited by the chemicalbook of Tian Ye.

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.

Originator

Tanabe Seiyaku (Japan)

Uses

Taltirelin is a thyrotropin-releasing hormone analog.

Uses

Analog of thyrotropin releasing hormone TRH, with pronounced CNS activity. Used in the treatment of spinocerebellar degeneration.

Definition

ChEBI: Taltirelin is an oligopeptide comprising of (4S)-1-methyl-2,6-dioxohexahydropyrimidine-4-carboxylic acid, L-histidine and L-prolinamide joined in sequence by peptide linkages. It is a thyrotropin-releasing hormone (TRH) analog. Its tetrahydrate form is approved in Japan for the treatment of spinal muscular atrophy. It has a role as a nootropic agent, a neuroprotective agent and an analgesic.

brand name

Ceredist

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

Taltirelin Suppliers

Global( 147)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Sigma Audley	+86-18336680971 +86-18126314766	nova@sh-teruiop.com	China	525	58
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
Shenzhen Nexconn Pharmatechs Ltd	+86-755-89396905 +86-15013857715	admin@nexconn.com	China	10248	58
Shaanxi Pioneer Biotech Co., Ltd .	+8613259417953	sales@pioneerbiotech.com	China	3000	58
Beijing Yibai Biotechnology Co., Ltd	0086-182-6772-3597	sales04@yibaibiotech.com	CHINA	419	58
Alchem Pharmtech,Inc.	8485655694	sales@alchempharmtech.com	United States	63711	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49390	58
career henan chemical co	+86-0371-86658258 15093356674;	factory@coreychem.com	China	29826	58
Fuxin Pharmaceutical	+86-021-021-50872116 +8613122107989	contact@fuxinpharm.com	China	10297	58
SIMAGCHEM CORP	+86-13806087780	sale@simagchem.com	China	17367	58

Supplier	Advantage
Sigma Audley	58
Capot Chemical Co.,Ltd.	60
Shenzhen Nexconn Pharmatechs Ltd	58
Shaanxi Pioneer Biotech Co., Ltd .	58
Beijing Yibai Biotechnology Co., Ltd	58
Alchem Pharmtech,Inc.	58
CONIER CHEM AND PHARMA LIMITED	58
career henan chemical co	58
Fuxin Pharmaceutical	58
SIMAGCHEM CORP	58

View Lastest Price from Taltirelin manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2024-01-17	Taltirelin 103300-74-9	US $25.00-15.00 / box	1box	99.9%	200tons/year	Sigma Audley
2023-11-27	Taltirelin 103300-74-9	US $0.00 / MG	10MG	99%	20 TONS	Wuhan Senwayer Century Chemical Co.,Ltd
2022-10-13	Taltirelin 103300-74-9	US $0.00-0.00 / kg	1kg	98%	1Ton	Henan Aochuang Chemical Co.,Ltd.

Taltirelin
103300-74-9
US $25.00-15.00 / box
99.9%
Sigma Audley

Taltirelin
103300-74-9
US $0.00 / MG
99%
Wuhan Senwayer Century Chemical Co.,Ltd

Taltirelin
103300-74-9
US $0.00-0.00 / kg
98%
Henan Aochuang Chemical Co.,Ltd.

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Taltirelin 5,6-DIHYDRO-6-METHYLURACIL taltirelin hydrate

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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