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Tocris/Sarpogrelate hydrochloride/3739/50/50 mg

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货号: 3739/50

品牌: Tocris

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Description: Selective 5-HT_2A antagonist

Alternative Names: MCI 9042

Chemical Name: Succinic acid mono-(1-dimethylaminomethyl-2-(2-[2-(3-methoxyphenyl)ethyl]phenoxy)ethyl) ester hydrochloride

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective 5-HT_2A receptor antagonist (pK_i values are 8.52, 7.43 and 6.57 for 5-HT_2A, 5-HT_2C and 5-HT_2B receptors respectively). Displays selectivity over 5-HT₁, 5-HT₃, 5-HT₄ H₁, H₂, M₃, α₁-adrenergic, α₂-adrenergic and β-adrenergic receptors. Displays cardioprotective activity in vivo.

Compound Libraries

Sarpogrelate hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	465.97
Formula	C₂₄H₃₁NO₆.HCl
Storage	Desiccate at RT
Purity	≥99% (HPLC)
CAS Number	135159-51-2
PubChem ID	444005
InChI Key	POQBIDFFYCYHOB-UHFFFAOYSA-N
Smiles	O=C(CCC(O)=O)OC(CN(C)C)COC1=CC=CC=C1CCC2=CC(OC)=CC=C2.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	46.6	100
	water	11.65	25

Preparing Stock Solutions

The following data is based on the product molecular weight 465.97. 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	2.15 mL	10.73 mL	21.46 mL
5 mM	0.43 mL	2.15 mL	4.29 mL
10 mM	0.21 mL	1.07 mL	2.15 mL
50 mM	0.04 mL	0.21 mL	0.43 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Rashid et al (2003) Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT₂ antagonist, to human 5-HT_2A, 5-HT_2B and 5-HT_2C receptor subtypes by molecular modeling. Life Sci. 73 193 PMID: 12738034

Brasil et al (2002) Blockade of 5-HT(2A) receptors by sarpogrelate protects the heart against myocardial infarction in rats. J.Cardiovasc.Pharmacol.Ther. 7 53 PMID: 12000979

Nishiyama (2009) Acute effects of sarpogrelate, a 5-HT_2A receptor antagonist on cytokine production in endotoxin shock model of rats. Eur.J.Pharmacol. 614 122 PMID: 19318092

Keywords: Sarpogrelate hydrochloride, supplier, MCI9042, selective, 5-HT2A, antagonists, receptors, serotonin, MCI, 9042, 5-HT2A, Receptors, 5-HT2A, Receptors, Tocris Bioscience

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