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SB 204741

  Cat. No.:  DC46455   Featured
Chemical Structure
152239-46-8
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More than 5000 active chemicals with high quality for research!
Field of application
SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 152239-46-8
Chemical Name: Urea,N-(1-methyl-1H-indol-5-yl)-N'-(3-methyl-5-isothiazolyl)-
Synonyms: Urea,N-(1-methyl-1H-indol-5-yl)-N'-(3-methyl-5-isothiazolyl)-;1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea;SB 204741;Lopac-S-0693;N-(1-Methyl-1H-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea;N-(1-Methyl-1H-indolyl-5-yl)-N''-(3-Methyl-5-isothiazolyl)urea;Tocris-1372;N-(1-Methyl-1H-5-indolyl)-N′-(3-methyl-5-isothiazolyl)urea;N-(1-METHYL-1H-5-INDOLYL)-N'-(3-METHYL-5-ISOTHIAZOLYL)UREA;1-(1-Methyl-1H-indol-5-yl)-3-(3-Methylisothiazol-5-yl)urea;N-(1-METHYL-1H-INDOLYL-5-YL)-N''-(3-METHYL-5-ISOTHIAZOLYL)UREA
SMILES: CN1C2C(=CC(NC(NC3SN=C(C)C=3)=O)=CC=2)C=C1
Formula: C14H14N4Os
M.Wt: 286.352160930634
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1].
Target: human 5-HT2B Receptor:7.1 (pKi)
In Vivo: SB-204741 (0.25~1.0 mg/kg; i.p.) induces myocardial remodeling and dose dependently improves hemodynamic and ventricular functions following isoproterenol-induced myocardial injury[1]. SB-204741 bolsters endogenous anti-oxidant enzymes activities, improves cardiac injury markers, NO level and lipid peroxidation level and attenuates TNFα level in isoproterenol-induced myocardial remodeling in rats. SB-204741 (0.5 and 1.0 mg/kg/day) pre-treatment for 28 days significantly amplifies NO level and GSH and SOD activities and attenuates TBARS level following isoproterenol-induced myocardial remodeling. SB-204741 inhibits inflammatory protein expression, upregulates autophagy and HSPs protein expressions in isoproterenol-induced myocardial remodeling in rats. SB-204741 improves myocardial architecture in isoproterenol-induced myocardial remodeling in rats[1]. Animal Model: Rats[1] Dosage: 0.25~1.0 mg/kg Administration: I.p. Result: Induced myocardial remodeling.
In Vitro: The most selective 5-HT2B receptor ligand to be tested is SB 204741 with approximately 20 fold selectivity for the human 5-HT2B receptor as compared to the human 5-HT2C receptor[1].
References: [1]. Bonhaus DW, et al. The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. Br J Pharmacol. 1995;115(4):622-628. [2]. Bharti S, et al. 5-HT2B receptor blockade attenuates β-adrenergic receptor-stimulated myocardial remodeling in rats via inhibiting apoptosis: role of MAPKs and HSPs. Apoptosis. 2015;20(4):455-465.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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