Biological Activity
Potent, selective 5-HT2 receptor antagonist; displays some selectivity for 5-HT2A receptors (Ki = 1.6 nM). IC50 values are 2.2, 310, 2400, 3700, > 5000 and > 5000 nM for 5-HT2, α1-adrenergic, D2 dopamine, 5-HT1, 5-HT3 and β-adrenergic receptors respectively. Inhibits 5-HT-induced platelet aggregation and pressor responses in vivo.
Compound Libraries
R-96544 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 391.94 |
| Formula | C22H29NO3.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 167144-80-1 |
| PubChem ID | 10668210 |
| InChI Key | OUKRSTJUAQEATQ-GZJHNZOKSA-N |
| Smiles | Cl[H].COC1=CC=CC(CCC2=C(OCC[C@@H]3C[C@@H](O)CN3C)C=CC=C2)=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 | 39.19 | 100 | |
| water | 39.19 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 391.94. 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 | 2.55 mL | 12.76 mL | 25.51 mL |
| 5 mM | 0.51 mL | 2.55 mL | 5.1 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.55 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Tanaka et al (2000) [2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding. Chem.Pharm.Bull. 48 1729 PMID: 11086903
Ogawa et al (2002) Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444. Eur.J.Pharmacol. 457 107 PMID: 12464356
Ogawa et al (2005) Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: additional evidence for possible involvement of 5-HT2A receptors in the development of expe Eur.J.Pharmacol. 521 156 PMID: 16183055
Keywords: R-96544 hydrochloride, supplier, Potent, selective, 5-HT2A, antagonists, serotonin, receptors, 5-HT2, antagonist, 5-HT2A, Receptors, 5-HT2A, Receptors, Tocris Bioscience
