RS 127445 hydrochloride

Pricing Availability   Qty
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)
Citations (8)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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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8 Citations for RS 127445 hydrochloride

Citations are publications that use Tocris products. Selected citations for RS 127445 hydrochloride include:

Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466 PMID: 24570000

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

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

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

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

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.