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Taltirelin

Taltirelin

CAS: 103300-74-9

Molecular Formula: C17H23N7O5

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Taltirelin - Names and Identifiers

Name Taltirelin
Synonyms TA 0910
Taltirelin
Ceredist, TA-0910
Taltirelin interMediate
TALTIRELIN INTERMEDIATES
Taltirelin Acetate,TA-0910
L-Prolinamide,(4S)-hexahydro-1-methyl-
2,6-dioxo-4-pyrimidinecarbonyl-L-histidyl-
(4S)-Hexahydro-1-Methyl-2,6-dioxo-4-pyriMidinecarbonyl-L-histidyl-
N-{[(4S)-1-methyl-2,6-dioxohexahydropyrimidin-4-yl]carbonyl}-L-histidyl-L-prolinamide
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)
(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
CAS 103300-74-9
InChI InChI=1/C17H23N7O5/c1-23-13(25)6-10(22-17(23)29)15(27)21-11(5-9-7-19-8-20-9)16(28)24-4-2-3-12(24)14(18)26/h7-8,10-12H,2-6H2,1H3,(H2,18,26)(H,19,20)(H,21,27)(H,22,29)/t10-,11-,12-/m0/s1

Taltirelin - Physico-chemical Properties

Molecular FormulaC17H23N7O5
Molar Mass405.41
Density1.447±0.06 g/cm3(Predicted)
Melting Point72-75°
Specific Rotation(α)25D -13.6° (c = 1 in water)
pKa9.32±0.40(Predicted)
Storage ConditionStore at +4°C
Refractive Index1.611

Taltirelin - Reference Information

, it was successfully developed by Mitsubishi Pharmaceutical Co., Ltd., Japan, and its trade name is taltielin. It belongs to the 3.1 class of new chemical drugs. At present, it is the most effective drug for improving the movement disorder of patients with spinocerebellar degeneration.
Taltirelin is the first approved oral thyrotropin-releasing hormone (TRH) in the world, it may also exert certain central nervous system (CNS) effects, including increased locomotor activity, antagonism of liserpin-induced hypothermia, and antagonism of pentobarbital-induced sleep. The variety was developed by Mitsubishi AG, Japan, and was first launched in Japan in September 2000. It is used to improve ataxia in patients with spinocerebellar degeneration. Spinocerebellar ataxia (SCAs), formerly known as autosomal dominant ataxia, is a group of chronic degenerative diseases of the central nervous system with ataxia and poor differentiation as the main clinical manifestations. Before September 2000, thyrotropin-releasing hormone (TRH) injection was the only drug used to treat this disease. Tatrierelin is a structural modification drug of TRH. Pharmacological studies have shown that this product produces strong and lasting multiple effects on the CNS via brain TRH receptors. The Excitatory effect of this product on CNS is 10~100 times stronger than TRH, and the duration of action is about 8 times longer than TRH. The affinity of this product to TRH receptor is about 1/11 of TRH, so the endocrine effect of this product is weaker than TRH, but this product is more stable than TRH in vivo. In addition, the effect of this product on the release of thyroid stimulating hormone (TSH) is 1/6-1/11 of TRH, and the release of TSH is regulated by a strong negative feedback system including thyroid hormone, has a strong effect on the central nervous system, but at the same time its hormone-like effect is small, so less side effects. Adverse reactions were mainly digestive system reactions, including Vomit, Nausea and stomach discomfort. All adverse reactions were mild to moderate and disappeared during treatment and/or after drug withdrawal.
oral thyrotropin-releasing hormone
biological activity taltielin (TA0910) is a thyrotropin-releasing hormone receptor (TRH-R) superagonist, the IC50 value was 910 nM and the EC50 value for stimulating an increase in cytosolic Ca2 concentration (Ca2 release) was 36 nM.
Target IC50: 910 nM
Last Update：2024-04-09 21:11:58
Taltirelin
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Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: Taltirelin Visit Supplier Webpage Request for quotation
CAS: 103300-74-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: Taltirelin Request for quotation
CAS: 103300-74-9
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: Taltirelin Visit Supplier Webpage Request for quotation
CAS: 103300-74-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Multiple SpecificationsSpot supply
Product Name: TA-0910 Visit Supplier Webpage Request for quotation
CAS: 103300-74-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
　　　　 tech@medchemexpress.com
Mobile: 609-228-6898
SKYRUN INDUSTRIAL CO.,LTD
Spot supply
Product Name: TALTIRELIN?INTERMEDIATES Visit Supplier Webpage Request for quotation
CAS: 103300-74-9
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185 Click to send a QQ messageSend QQ message
Wechat: chinaskyrun
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Taltirelin
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