R-96544 hydrochloride

Name: R-96544 hydrochloride
Brand: Tocris Bioscience
SKU: 1742

Catalog # 1742 | Tocris Bioscience a Bio-Techne Brand

Citations (3)

COA / SDS

Potent, selective 5-HT2A antagonist

Key Product Details

Description:	Potent, selective 5-HT_2A antagonist
Chemical Name:	(2R,4R)-5-[2-[2-[2-(3-Methoxyphenyl)ethyl]phenoxy]ethyl]-1-methyl-3-pyrrolidinol hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	391.94

View Full Technical Details for R-96544 hydrochloride

Technical Data
Citations (3) / Reviews

Biological Activity for R-96544 hydrochloride

R-96544 hydrochloride is a potent, selective 5-HT₂ receptor antagonist; displays some selectivity for 5-HT_2A receptors (K_i = 1.6 nM). IC₅₀ values are 2.2, 310, 2400, 3700, > 5000 and > 5000 nM for 5-HT₂, α₁-adrenergic, D₂ dopamine, 5-HT₁, 5-HT₃ and β-adrenergic receptors respectively. Inhibits 5-HT-induced platelet aggregation and pressor responses in vivo.

Compound Libraries for R-96544 hydrochloride

R-96544 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for R-96544 hydrochloride

M. Wt	391.94
Formula	C₂₂H₂₉NO₃.HCl
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	167144-80-1
PubChem ID	10668210
InChi Key	OUKRSTJUAQEATQ-GZJHNZOKSA-N
Smiles	Cl[H].COC1=CC=CC(CCC2=C(OCC[C@@H]3C[C@@H](O)CN3C)C=CC=C2)=C1

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 for R-96544 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	39.19	100
	DMSO	39.19	100

Preparing Stock Solutions for R-96544 hydrochloride

The following data is based on the product molecular weight 391.94.

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	2.55 mL	12.76 mL	25.51 mL
5 mM	0.51 mL	2.55 mL	5.10 mL
10 mM	0.26 mL	1.28 mL	2.55 mL
50 mM	0.05 mL	0.26 mL	0.51 mL

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References for R-96544 hydrochloride

References are publications that support the biological activity of the product.

Ogawa Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: additional evidence for possible involvement of 5-HT2A receptors in the development of expe Eur.J.Pharmacol. 2005 PMID: 16183055
Ogawa Pharmacological profiles of R-96544, the active form of a novel 5-HT_2A receptor antagonist R-102444. Eur.J.Pharmacol. 2002 PMID: 12464356
Tanaka [2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding. Chem.Pharm.Bull. 2000 PMID: 11086903

Citations for R-96544 hydrochloride (3)

Showing 1 - 3 of 3 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for R-96544 hydrochloride include:

Chien and Su (2015) 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts. PLoS One. 22:42
PMID: 26076928
Tanaka et al. (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem. 289:10466
PMID: 24570000
Xu et al. (2012) Deficits in LTP induction by 5-HT2A receptor antagonist in a mouse model for fragile X syndrome. J Pharmacol Exp Ther. 7:e48741
PMID: 23119095

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