RS 127445 hydrochloride

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Cat.No. 2993 - RS 127445 hydrochloride | C17H16FN3.HCl | CAS No. 199864-86-3
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)
Datasheet
Citations (8)
Reviews
Literature (3)

Biological Activity

High affinity 5-HT2B receptor antagonist (pKi = 9.5). Displays 1000-fold selectivity for 5-HT2B with good bioavailability.

Compound Libraries

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.78 100
ethanol 31.78 100

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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:

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

Söhle et al (2012) Identification of new genes involved in human adipogenesis and fat storage. PLoS One 7 e31193 PMID: 22384002

Moutkine et al (2017) Heterodimers of serotonin receptor subtypes 2 are driven by 5-HT2C protomers. J Biol Chem 292 6352 PMID: 28258217


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Literature in this Area

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