All Photos(1)
Synonym(s):
1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine
Empirical Formula (Hill Notation):
C16H22N4O4S
Recommended Products
Quality Level
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.).
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Information
监管及禁止进口产品
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
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
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
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.
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
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%
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
Contact Technical Service