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Merck
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文件

SML2905

Sigma-Aldrich

Rovatirelin

≥98% (HPLC)

别名:

1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine

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About This Item

经验公式（希尔记法）:
C16H22N4O4S
CAS号:
204386-76-5
分子量:
366.44
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

2-8°C

InChI

1S/C16H22N4O4S/c1-9-4-3-5-20(9)15(22)12(6-11-7-25-8-17-11)18-14(21)13-10(2)24-16(23)19-13/h7-10,12-13H,3-6H2,1-2H3,(H,18,21)(H,19,23)/t9-,10+,12+,13+/m1/s1

InChI 密鑰

WTXWDXWZGJGIHV-URBCHYCLSA-N

生化／生理作用

Rovatirelin is an orally active and brain-penetrant thyrotropin-releasing hormone (TRH) mimetic with higher receptor affinity than taltirelin (Ki = 702 nM vs 3877 nM, repectively). Rovatirelin oral administration in rats (10 or 30 mg/kg p.o.) upregulates locus coeruleus (LC) c-Fos expression and medial prefrontal cortex (mPFC) extracellular noradrenaline (NA), being more potent than taltirelin in enhancing spontaneous firing activity of isolated rat LC noradrenergic neurons in vitro (10-1000 nM) and rat locomotor activity in vivo (10 or 30 mg/kg p.o.).

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

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Kaoru Kobayshi et al.
Xenobiotica; the fate of foreign compounds in biological systems, 49(12), 1434-1446 (2019-02-13)
The mass balance, pharmacokinetics and metabolism of rovatirelin were characterised in healthy male subjects after a single oral dose of [14C]rovatirelin. [14C]Rovatirelin was steadily absorbed, and the peak concentrations of radioactivity and rovatirelin were observed in plasma at 5-6 h after
Tomoyuki Ijiro et al.
European journal of pharmacology, 761, 413-422 (2015-07-06)
Rovatirelin ([1-[-[(4S,5S)-(5-methyl-2-oxo oxazolidin-4-yl) carbonyl]-3-(thiazol-4-yl)-l-alanyl]-(2R)-2-methylpyrrolidine) is a novel synthetic agent that mimics the actions of thyrotropin-releasing hormone (TRH). The aim of this study was to investigate the electrophysiological and pharmacological effects of rovatirelin on the central noradrenergic system and to compare
Kaoru Kobayashi et al.
Xenobiotica; the fate of foreign compounds in biological systems, 49(1), 106-119 (2018-01-05)
1. The non-clinical pharmacokinetic profiles of rovatirelin, a novel thyrotropin-releasing hormone (TRH) analogue, were investigated in vivo and in vitro. 2. Rovatirelin orally administered to rats and dogs was rapidly absorbed and bioavailability was estimated to be 7.3 and 41.3%
Naotake Kobayashi et al.
Journal of peptide science : an official publication of the European Peptide Society, 25(12), e3228-e3228 (2019-11-13)
We discovered the orally active thyrotropin-releasing hormone (TRH) mimetic: (4S,5S)-5-methyl-N-{(2S)-1-[(2R)-2-methylpyrrolidin-1-yl]-1-oxo-3-(1,3-thiazol-4-yl)propan-2-yl}-2-oxo-1,3-oxazolidine-4-carboxamide 1 (rovatirelin). The central nervous system (CNS) effect of rovatirelin after intravenous (iv) administration is 100-fold higher than that of TRH. As 1 has four asymmetric carbons in its molecule
Naotake Kobayashi et al.
ACS omega, 3(10), 13647-13666 (2018-11-10)
We have explored orally effective thyrotropin-releasing hormone (TRH) mimetics, showing oral bioavailability and brain penetration by structure-activity relationship (SAR) study on the basis of in vivo antagonistic activity on reserpine-induced hypothermia in mice. By primary screening of the synthesized TRH

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