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SML2905

Sigma-Aldrich

Rovatirelin

≥98% (HPLC)

Synonyma:

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

Empirický vzorec (Hillův zápis):
C16H22N4O4S
Číslo CAS:
204386-76-5
Molekulová hmotnost:
366.44
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

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 key

WTXWDXWZGJGIHV-URBCHYCLSA-N

Biochem/physiol Actions

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.).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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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
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
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
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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