产品说明书

Sarpogrelate HCl

Print
Chemical Structure| 135159-51-2 同义名 : MCI-9042;Sarpogrelate (hydrochloride);Sarpogrelate hydrochloride
CAS号 : 135159-51-2
货号 : A166685
分子式 : C24H32ClNO6
纯度 : 98%
分子量 : 465.967
MDL号 : MFCD00887582
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(128.76 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 30 mg/mL(64.38 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • 5-HT2

    5-HT2C, Kd:1.1 nM

    5-HT2A, Kd:2.1 nM
描述 Sarpogrelate Hydrochloride is a highly selective serotonin (5-hydroxytryptamine, 5-HT2A) receptor antagonist used as an antiplatelet agent for the treatment of peripheral artery disease. Sarpogrelate hydrochloride might be a weak inhibitor of CYP (cytochrome P450 ) 2D6[3]. Moreover, Sarpogrelate Hydrochloride ameliorates diabetic nephropathy not only by suppressing macrophage infiltration, but also by anti-inflammatory and anti-fibrotic effects[4]. A 5- or 1-day treatment with 50 mg/kg sarpogrelate can completely protect the retina of BALB/c mice from light-induced retinopathy[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.73mL

2.15mL

1.07mL

21.46mL

4.29mL

2.15mL
参考文献

[1]Nishio H, Inoue A, et al. Binding affinity of sarpogrelate, a new antiplatelet agent, and its metabolite for serotonin receptor subtypes. Arch Int Pharmacodyn Ther. 1996 Mar-Apr;331(2):189-202.

[2]Pertz H, Elz S. 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 Pharmacol. 1995 Apr;47(4):310-6.

[3]Min JS, Kim D, Park JB, Heo H, Bae SH, Seo JH, Oh E, Bae SK. Application of physiologically based pharmacokinetic modeling in predicting drug-drug interactions for sarpogrelate hydrochloride in humans. Drug Des Devel Ther. 2016 Sep 14;10:2959-2972. doi: 10.2147/DDDT.S109141. PMID: 27695293; PMCID: PMC5028085.

[4]Lee ES, Lee MY, Kwon MH, Kim HM, Kang JS, Kim YM, Lee EY, Chung CH. Sarpogrelate hydrochloride ameliorates diabetic nephropathy associated with inhibition of macrophage activity and inflammatory reaction in db/db mice. PLoS One. 2017 Jun 22;12(6):e0179221. doi: 10.1371/journal.pone.0179221. PMID: 28640832; PMCID: PMC5480859.

[5]Tullis BE, Ryals RC, Coyner AS, Gale MJ, Nicholson A, Ku C, Regis D, Sinha W, Datta S, Wen Y, Yang P, Pennesi ME. Sarpogrelate, a 5-HT2A Receptor Antagonist, Protects the Retina From Light-Induced Retinopathy. Invest Ophthalmol Vis Sci. 2015 Jul;56(8):4560-9. doi: 10.1167/iovs.15-16378. PMID: 26200496; PMCID: PMC4515947.