RS 127445 hydrochloride

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Cat.No. 2993 - RS 127445 hydrochloride | C17H16FN3.HCl | CAS No. 199864-86-3
Description: Selective, high affinity 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 (3)
Reviews
Literature

Biological Activity

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

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.

All Tocris products are intended for laboratory research use only.

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 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 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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Safety Datasheet

References

References are publications that support the products' biological activity.

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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3 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

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

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


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