Biological Activity
Potent and selective 5-HT2B receptor antagonist (pA2 = 7.95). Displays ≥ 135-fold selectivity over 5-HT2C (pKi = 5.82), 5-HT2A (pKi < 5.2), 5-HT1A, 1D, 1E, 5-HT3 and 5-HT4 receptors.
Licensing Information
Sold under license
Technical Data
| M. Wt | 286.35 |
| Formula | C14H14N4OS |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 152239-46-8 |
| PubChem ID | 3277600 |
| InChI Key | USFUFHFQWXDVMH-UHFFFAOYSA-N |
| Smiles | O=C(NC3=CC(C)=NS3)NC1=CC(C=CN2C)=C2C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.64 | 100 | |
| ethanol | 5.73 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 286.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.49 mL | 17.46 mL | 34.92 mL |
| 5 mM | 0.7 mL | 3.49 mL | 6.98 mL |
| 10 mM | 0.35 mL | 1.75 mL | 3.49 mL |
| 50 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bonhaus et al (1995) The pharmacology and distribution of human 5-hydroxytryptamine2B (5-HT2B) receptor gene products: comparison with 5-HT2A and 5-HT2C receptors. Br.J.Pharmacol. 115 622 PMID: 7582481
Forbes et al (1995) N-(1-Methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist. J.Med.Chem. 38 855 PMID: 7699699
Glusa and Pertz (2000) Further evidence that 5-HT-induced relaxation of pig pulmonary artery is mediated by endothelial 5-HT2B receptors. Br.J.Pharmacol. 130 692 PMID: 10821800
Ebrahimkhani et al (2011) Stimulating healthy tissue regeneration by targeting the 5-HT2B receptor in chronic liver disease. Nat.Med. 17 1668 PMID: 22120177
Keywords: SB 204741, supplier, Potent, selective, 5-HT2B, antagonists, Serotonin, Receptors, SB204741, 5-HT2B, Receptors, 5-HT2B, Receptors, Tocris Bioscience
