CAS 152239-46-8|SB 204741
| Common Name | SB 204741 | ||
|---|---|---|---|
| CAS Number | 152239-46-8 | Molecular Weight | 286.35200 |
| Density | 1.38g/cm3 | Boiling Point | 335.9ºC at 760 mmHg |
| Molecular Formula | C14H14N4OS | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 157ºC |
| Symbol | GHS07 | Signal Word | Warning |
Names
| Name | 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea |
|---|---|
| Synonym | More Synonyms |
SB 204741 BiologicalActivity
| Description | SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1]. |
|---|---|
| Related Catalog | Research 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 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. |
Chemical & Physical Properties
| 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 |
| InChIKey | USFUFHFQWXDVMH-UHFFFAOYSA-N |
| SMILES | Cc1cc(NC(=O)Nc2ccc3c(ccn3C)c2)sn1 |
| Storage condition | 2-8°C |
Safety Information
| Symbol | 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 |
Articles1
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Synonyms
| Tocris-1372 |
| N-(1-Methyl-1H-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea |
| Lopac-S-0693 |
