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152239-46-8

152239-46-8 structure
152239-46-8 structure
  • Name: SB 204741
  • Chemical Name: 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea
  • CAS Number: 152239-46-8
  • Molecular Formula: C14H14N4OS
  • Molecular Weight: 286.35200
  • Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
  • Create Date: 2018-12-24 17:01:02
  • Modify Date: 2024-01-14 18:25:01
  • SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1].

Name 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea
Synonyms Tocris-1372
N-(1-Methyl-1H-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea
Lopac-S-0693
Description SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1].
Related Catalog
Target

human 5-HT2B Receptor:7.1 (pKi)

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].
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.
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.

Density 1.38g/cm3
Boiling Point 335.9ºC at 760 mmHg
Molecular Formula C14H14N4OS
Molecular Weight 286.35200
Flash Point 157ºC
Exact Mass 286.08900
PSA 87.19000
LogP 3.73320
Vapour Pressure 0.000116mmHg at 25°C
Index of Refraction 1.707
Storage condition 2-8°C
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
RIDADR NONH for all modes of transport