| Identification | Back Directory | [Name]
SB 204741 | [CAS]
152239-46-8 | [Synonyms]
SB 204741
1-(1-methyl-5-indolyl)-3-(3-methyl-5-isothiazolyl)urea
3-(3-METHYL-1,2-THIAZOL-5-YL)-1-(1-METHYLINDOL-5-YL)UREA
1-(1-Methyl-1H-indol-5-yl)-3-(3-Methylisothiazol-5-yl)urea
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
Urea, N-(1-methyl-1H-indol-5-yl)-N'-(3-methyl-5-isothiazolyl)- | [Molecular Formula]
C14H14N4OS | [MDL Number]
MFCD00923644 | [MOL File]
152239-46-8.mol | [Molecular Weight]
286.35 |
| Chemical Properties | Back Directory | [Melting point ]
>195°C (dec.) | [storage temp. ]
2-8°C
| [solubility ]
DMSO: ~18 mg/mL, soluble
| [form ]
solid
| [color ]
orange
| [Stability:]
Hygroscopic |
| Hazard Information | Back Directory | [Uses]
SB 204741 is a potent, selective SR-2B antagonist. | [Definition]
ChEBI: 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea is a member of ther class of ureas that is urea in which a hydrogen attached to one of the nitrogens has been replaced by an N-methylindol-5-yl group, while a hydrogen attached to the other nitrogen has been replaced by a 3-methyl-1,2-thiazol-5-yl group. It is a potent and selective antagonist for the 5-hydroxytryptamine 2B (5-HT2B) receptor. It has a role as a receptor modulator and a serotonergic antagonist. It is a member of ureas, a member of indoles and a member of 1,2-thiazoles. | [Biological Activity]
Potent and selective 5-HT 2B receptor antagonist (pA 2 = 7.95). Displays ≥ 135-fold selectivity over 5-HT 2C (pK i = 5.82), 5-HT 2A (pK i < 5.2), 5-HT 1A , 1D , 1E , 5-HT 3 and 5-HT 4 receptors. | [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.
|
| [IC 50]
human 5-HT2B Receptor: 7.1 (pKi) | [storage]
Store at 2-8℃ |
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