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Sarpogrelate hydrochloride

Catalog No. T4978 CAS 135159-51-2

Synonyms: MCI-9042

Sarpogrelate hydrochloride (MCI-9042) , a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. Target: 5-HT2 Recepter Sarpogrelate is a drug which acts as an antagonist at the 5HT2A and 5-HT2B receptors. Sarpogrelate hydrochloride was shown to have the same affinity as ritanserin for 5-HT2A receptors, with a Ki value of 8.39 nM. Sarpogrelate hydrochloride lacked prominent 5-HT1-like, 5-HT3, beta, H1, H2 and M3 antagonist activity and weakly blocked alpha 1-adrenoceptors (pKB = 6.30). (S)-M-1 showed weak affinity for 5-HT1-like receptors (pKB = 6.30), alpha 1- (pKB = 6.80) and beta- (pKB = 6.54) adrenoceptors, while (R)-M-1 was a weak antagonist at histamine H1 receptors (pKB = 6.49). After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate hydrochloride -induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. Long-term oral administration of sarpogrelate improves vascular function in patients with PAD.

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Sarpogrelate hydrochloride Chemical Structure

Sarpogrelate hydrochloride, CAS 135159-51-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 41.00
10 mg	In stock	$ 66.00
25 mg	In stock	$ 122.00
50 mg	In stock	$ 195.00
100 mg	In stock	$ 288.00
500 mg	In stock	$ 688.00
1 mL * 10 mM (in DMSO)	In stock	$ 47.00

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Purity: 99.42%

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Description

Targets&IC50

5-HT2A:8.39 nM(Ki)

Synonyms	MCI-9042
Molecular Weight	465.97
Formula	C24H32ClNO6
CAS No.	135159-51-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 46.6 mg/mL(100 mM)

References and Literature

1. Pertz, H. and S. Elz, In-vitro pharmacology of sarpogrelate and the enantiomers of its major metabolite: 5-HT2A receptor specificity, stereoselectivity and modulation of ritanserin-induced depression of 5-HT contractions in rat tail artery. J Pharm Pharma 2. Miyazaki, M., et al., Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease. J Cardiovasc Pharmacol, 2007. 49(4): p. 221-7. 3. Nishio, H., A. Inoue, and Y. Nakata, Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Arch Int Pharmacodyn Ther, 1996. 331(2): p. 189-202.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library GPCR Compound Library Drug Repurposing Compound Library Anti-COVID-19 Compound Library Neuronal Signaling Compound Library Anti-Parkinson's Disease Compound Library

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Keywords

Sarpogrelate hydrochloride 135159-51-2 GPCR/G Protein Neuroscience 5-HT Receptor vascular 5-HT2R Inhibitor inhibit MCI9042 thrombosis MCI-9042 Sarpogrelate Hydrochloride 5-hydroxytryptamine Receptor Sarpogrelate Serotonin Receptor MCI 9042 inhibitor

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