CAS 152239-46-8|SB 204741

Introduction:Basic information about CAS 152239-46-8|SB 204741, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameSB 204741
CAS Number152239-46-8Molecular Weight286.35200
Density1.38g/cm3Boiling Point335.9ºC at 760 mmHg
Molecular FormulaC14H14N4OSMelting Point/
MSDSChineseUSAFlash Point157ºC
Symbol
GHS07
Signal WordWarning

Names

Name1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea
SynonymMore Synonyms

SB 204741 BiologicalActivity

DescriptionSB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1].
Related CatalogResearch Areas >>Cardiovascular DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor
Target

human 5-HT2B Receptor:7.1 (pKi)

In VitroThe 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].
In VivoSB-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.
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.

Chemical & Physical Properties

Density1.38g/cm3
Boiling Point335.9ºC at 760 mmHg
Molecular FormulaC14H14N4OS
Molecular Weight286.35200
Flash Point157ºC
Exact Mass286.08900
PSA87.19000
LogP3.73320
Vapour Pressure0.000116mmHg at 25°C
Index of Refraction1.707
InChIKeyUSFUFHFQWXDVMH-UHFFFAOYSA-N
SMILESCc1cc(NC(=O)Nc2ccc3c(ccn3C)c2)sn1
Storage condition2-8°C

Safety Information

Symbol
GHS07
Signal WordWarning
Hazard StatementsH315-H319-H335
Precautionary StatementsP261-P305 + P351 + P338
Personal Protective Equipmentdust mask type N95 (US);Eyeshields;Gloves
RIDADRNONH for all modes of transport

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Synonyms

Tocris-1372
N-(1-Methyl-1H-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea
Lopac-S-0693
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CAS 145307-34-2|A 77636 hydrochloride
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