
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 152239-46-8 |
| Catalog No. | 2A-9083015 |
| Chinese Name | SB 204741,5-HT 2B受体拮抗剂 |
| Synonyms | Tocris-1372; N-(1-Methyl-1H-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea; Lopac-S-0693 |
| Molecular Formula | C14H14N4OS |
| Molecular Weight | 286.35 |
| Purity | >98 (HPLC) |
| Density | 1.38g/cm3 |
| Boiling Point | 335.9ºC at 760 mmHg |
| Appearance | solid |
| Storage Condition | 2-8°C |
| Application | SB 204741 is a selective, high-affinity 5-HT2B antagonist with a pKi value of 7.1[1]. |
| PubChem ID | 24278321 |
| MDL Number | MFCD00923644 |
| SMILES | Cc1cc(NC(=O)Nc2ccc3n(C)ccc3c2)sn1 |
| InChI | 1S/C14H14N4OS/c1-9-7-13(20-17-9)16-14(19)15-11-3-4-12-10(8-11)5-6-18(12)2/h3-8H,1-2H3,(H2,15,16,19) |
| InChI Key | USFUFHFQWXDVMH-UHFFFAOYSA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| Hazard Symbols | transportation |
| MSDS | msds/83015_1_152239_46_8.pdf |
| Bioactivity | SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1]. Related Catalog Research Areas >> Cardiovascular Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling 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 |
| Use of | SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1[1]. Properties Name 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea Synonym More Synonyms SB 204741 Biological Activity 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 Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor human 5-HT2B Receptor:7.1 (pKi) References [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 Molecular Formula C14H14N4OS Exact Mass 286.08900 PSA 87.19000 LogP 3.73320 Index of Refraction 1.707 InChIKey USFUFHFQWXDVMH-UHFFFAOYSA-N |
| Transport Info | Product name: Purity: 99.0% |
| MSDS Transport Info | Module 14. Shipping information 14.1 UN number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 Names specified by the United Nations (UN) European Land Transport Dangerous Regulations: No dangerous goods IMDG Code: No dangerous goods International Air Transport Dangerous Regulations: No dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Dangerous Regulations: No International Maritime Transport Dangerous Regulations Maritime Pollutants: No International Air Transport Risk Regulations: No 14.6 Special precautions for users No data available |
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