RS 127445 hydrochloride

Catalog #: 2993
8 Citations Datasheet / COA / SDS

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RS 127445 hydrochloride | CAS No. 199864-86-3 | 5-HT2B Receptor Antagonists

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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%

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Product Details

Citations (8)

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Biological Activity

RS 127445 hydrochloride is a high affinity 5-HT_2B receptor antagonist (pK_i = 9.5). Displays 1000-fold selectivity for 5-HT_2B with good bioavailability.

Technical Data

M.Wt:

317.79

Formula:

C₁₇H₁₆FN₃.HCl

Solubility:

Soluble to 100 mM in DMSO and to 100 mM in ethanol

Purity:

≥98%

Storage:

Desiccate at +4°C

CAS No:

199864-86-3

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.

Background References

Identification of new genes involved in human adipogenesis and fat storage.
Sohle J, Machuy N, Smailbegovic E, Holtzmann U, Gronniger E, Wenck H, Stab F, Winnefeld M
PLoS ONE, 2012;7(2):e31193.
RS-127445: a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist.
Bonhaus et al.
Br.J.Pharmacol., 1999;127:1075
Evidence for a control of plasma serotonin levels by 5-Hydroxytryptamine_2B receptors in mice.
Callebert et al.
J.Pharmacol.Exp.Ther., 2006;317:724

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Citations for RS 127445 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for RS 127445 hydrochloride include:

8 Citations: Showing 1 - 8

Pulmonary fibrosis in vivo displays increased p21 expression reduced by 5-HT2B receptor antagonists in vitro - a potential pathway affecting proliferation.
Authors: Lofdahl
Sci Rep 2018;8(1):1927
Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers.
Authors: Moutkine Et al.
J Biol Chem 2017;292:6352
A human and animal model-based approach to investigating the anti-inflammatory profile and potential of the 5-HT2B receptor antagonist AM1030.
Authors: Palmqvist Et al.
J Inflamm (Lond) 2016;13:20
Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells.
Authors: Tanaka Et al.
J Biol Chem 2014;289:10466
Serotonin 2B receptor (5-HT2B R) signals through prostacyclin and PPAR-β/δ in osteoblasts.
Authors: Chabbi-Achengli Et al.
PLoS One 2013;8:e75783
Identification of new genes involved in human adipogenesis and fat storage.
Authors: Söhle Et al.
PLoS One 2012;7:e31193
Deconstructing antiobesity compound action: requirement of serotonin 5-HT2B receptors for dexfenfluramine anorectic effects.
Authors: Banas Et al.
Neuropsychopharmacology 2011;36:423
Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors.
Authors: Murray Et al.
J Neurophysiol 2011;106:925

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