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Submit ReviewRS 127445 hydrochloride
Description: High affinity and selective 5-HT2B antagonist
Alternative Names: MT 500
Chemical Name: 4-(4-Fluoro-1-naphthalenyl)-6-(1-methylethyl)-2-pyrimidinamine hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for RS 127445 hydrochloride
RS 127445 hydrochloride is a high affinity 5-HT2B receptor antagonist (pKi = 9.5). Displays 1000-fold selectivity for 5-HT2B with good bioavailability.
Compound Libraries for RS 127445 hydrochloride
RS 127445 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for RS 127445 hydrochloride
| M. Wt | 317.79 |
| Formula | C17H16FN3.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 199864-86-3 |
| PubChem ID | 9905058 |
| InChI Key | MKJPYBJBPRFMHL-UHFFFAOYSA-N |
| Smiles | FC1=C(C=CC=C2)C2=C(C3=CC(C(C)C)=NC(N)=N3)C=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RS 127445 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.78 | 100 | |
| ethanol | 31.78 | 100 |
Preparing Stock Solutions for RS 127445 hydrochloride
The following data is based on the product molecular weight 317.79. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 3.15 mL | 15.73 mL | 31.47 mL |
| 5 mM | 0.63 mL | 3.15 mL | 6.29 mL |
| 10 mM | 0.31 mL | 1.57 mL | 3.15 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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Product Datasheets for RS 127445 hydrochloride
References for RS 127445 hydrochloride
References are publications that support the biological activity of the product.
Bonhaus et al (1999) RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br.J.Pharmacol. 127 1075 PMID: 10455251
Callebert et al (2006) Evidence for a control of plasma serotonin levels by 5-Hydroxytryptamine2B receptors in mice. J.Pharmacol.Exp.Ther. 317 724 PMID: 16461587
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Keywords: RS 127445 hydrochloride, RS 127445 hydrochloride supplier, Selective, high, affinity, 5-HT2B, antagonists, Serotonin, Receptors, RS127445, hydrochloride, MT500, MT, 500, 2993, Tocris Bioscience
8 Citations for RS 127445 hydrochloride
Citations are publications that use Tocris products. Selected citations for RS 127445 hydrochloride include:
Söhle et al (2012) Identification of new genes involved in human adipogenesis and fat storage. PLoS One 7 e31193 PMID: 22384002
Lofdahl (2018) Pulmonary fibrosis in vivo displays increased p21 expression reduced by 5-HT2B receptor antagonists in vitro - a potential pathway affecting proliferation. Sci Rep 8 1927 PMID: 29386571
Palmqvist et al (2016) A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030. J Inflamm (Lond) 13 20 PMID: 27340371
Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466 PMID: 24570000
Chabbi-Achengli et al (2013) Serotonin 2B receptor (5-HT2B R) signals through prostacyclin and PPAR-β/δ in osteoblasts. PLoS One 8 e75783 PMID: 24069449
Moutkine et al (2017) Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers. J Biol Chem 292 6352 PMID: 28258217
Banas et al (2011) Deconstructing antiobesity compound action: requirement of serotonin 5-HT2B receptors for dexfenfluramine anorectic effects. Neuropsychopharmacology 36 423 PMID: 20927048
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
Do you know of a great paper that uses RS 127445 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.