货号:A166685
同义名:
MCI-9042; Sarpogrelate (hydrochloride)
Sarpogrelate HCl 是一种 5-HT₂A 和 5-HT₂B 受体拮抗剂,可阻断血清素诱导的血小板聚集,常用于糖尿病、Buerger 病、雷诺病、冠状动脉病、心绞痛和动脉粥样硬化的研究。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
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| 产品名称 | 5-HT ↓ ↑ | 5-HT1 ↓ ↑ | 5-HT2 ↓ ↑ | 5-HT3 ↓ ↑ | 5-HT5 ↓ ↑ | 5-HT6 ↓ ↑ | 5-HT7 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Desvenlafaxine |
++
5-HT, Ki: 40.2 nM |
98% | |||||||||||||||||
| Lamotrigine |
+
5-HT (rat brain synaptosomes), IC50: 474 μM 5-HT (human platelets), IC50: 240 μM |
98% | |||||||||||||||||
| Venlafaxine | ✔ | 99% | |||||||||||||||||
| Fluvoxamine maleate | ✔ | 99% | |||||||||||||||||
| Iloperidone | ✔ | 99% | |||||||||||||||||
| Ziprasidone HCl | ✔ | 98+% | |||||||||||||||||
| Atomoxetine HCI |
+
5-HT, Ki: 77 nM |
98% | |||||||||||||||||
| Dapoxetine HCl | ✔ | 97% | |||||||||||||||||
| Trazodone | ✔ | 98+% | |||||||||||||||||
| Clomipramine HCl | ✔ | 98% | |||||||||||||||||
| Mirtazapine | ✔ | 99+% | |||||||||||||||||
| Escitalopram oxalate |
+++
5-HT, Ki: 0.89 nM |
97% | |||||||||||||||||
| Duloxetine | ✔ | 97% | |||||||||||||||||
| Sertraline HCl |
++
5-HT, Ki: 13 nM |
98% | |||||||||||||||||
| Citalopram HBr |
+++
serotonin reuptake, IC50: 1.8 nM |
98% | |||||||||||||||||
| Latrepirdine 2HCl | ✔ | GluR | 99% | ||||||||||||||||
| Fluoxetine HCl | ✔ | 99.5% | |||||||||||||||||
| Paroxetine HCl | ✔ | AChR | 99% | ||||||||||||||||
| BMY 7378 |
++
5-HT1A, pIC50: 6.4 5-HT1D, pIC50: 5.9 |
+
5-HT2, pIC50: 5.5 |
97% | ||||||||||||||||
| Flibanserin |
+++
5-HT1A, Ki: 1 nM |
+
5-HT2A, Ki: 49 nM |
95% | ||||||||||||||||
| LY310762 |
+
5-HT1D, Ki: 249 nM |
99%+ | |||||||||||||||||
| Cyclobenzaprine HCI | ✔ | 99% | |||||||||||||||||
| Blonanserin |
+++
5-HT2, Ki: 3.98 nM |
99% | |||||||||||||||||
| Cyproheptadine HCl |
++++
5-HT2, IC50: 0.6 nM |
99+% | |||||||||||||||||
| Olanzapine | ✔ | 99+% | |||||||||||||||||
| Pimavanserin hemitartrate |
+++
5-HT2A, pIC50: 8.7 |
99% | |||||||||||||||||
| Ketanserin |
+++
5-HT2C (Human), Ki: 2.5 nM 5-HT2C (Rat), Ki: 50 nM |
99%+ | |||||||||||||||||
| Loxapine succinate |
++
5-HT2 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 nM |
98% | |||||||||||||||||
| Agomelatine | ✔ | 98% | |||||||||||||||||
| Clozapine | ✔ | 98% | |||||||||||||||||
| Amitriptyline |
+
5-HT2, Ki: 235 nM |
SERT | 99% | ||||||||||||||||
| PRX-08066 maleate |
+++
5-HT2B, IC50: 3.4 nM |
98+% | |||||||||||||||||
| RS-127445 |
++++
5-HT2B, pIC50: 10.4 5-HT2B, pKi: 9.5 |
99%+ | |||||||||||||||||
| Sarpogrelate HCl |
++++
5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 nM |
98% | |||||||||||||||||
| Tropisetron | ✔ | 99% | |||||||||||||||||
| Ramosetron HCl |
++++
5-HT3 receptor, Ki: 0.091 nM |
98% | |||||||||||||||||
| Ondansetron | ✔ | 99% | |||||||||||||||||
| Granisetron | ✔ | 98% | |||||||||||||||||
| Alosetron HCl | ✔ | 98% | |||||||||||||||||
| Ondansetron HCl dihydrate | ✔ | 98% | |||||||||||||||||
| VUF10166 |
++++
5-HT3A, Ki: 0.04 nM 5-HT3AB, Ki: 22 nM |
99%+ | |||||||||||||||||
| Azasetron HCl |
++++
5-HT3, IC50: 0.33 nM |
99% | |||||||||||||||||
| Asenapine maleate |
+++
5-HT1B, pKi: 8.4 5-HT1A, pKi: 8.6 |
++++
5-HT2A, pKi: 9.75 5-HT2C, pKi: 10.46 |
+++
5-HT5A, pKi: 8.84 |
++++
5-HT6, pKi: 9.6 |
++++
5-HT7, pKi: 9.94 |
97% | |||||||||||||
| Risperidone |
++
5-HT1D, Ki: 84.6 nM 5-HT1B, Ki: 14.9 nM |
++++
5-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 nM |
+
5-HT5A, Ki: 206 nM |
++
5-HT7, Ki: 6.6 nM |
98% | ||||||||||||||
| SB 271046 HCl |
+++
5-HT6, pKi: 8.92 |
99%+ | |||||||||||||||||
| Intepirdine |
++++
5-HT6, pKi: 9.63 |
99%+ | |||||||||||||||||
| SB-269970 HCl |
++
5-HT7, pKi: 8.3 |
98+% | |||||||||||||||||
| BRL 15572 |
++
5-HT1D, pKi: 6 5-HT1B, pKi: 6.1 |
++
5-HT2A, pKi: 6.6 5-HT2B, pKi: 6.2 |
+
5-HT6, pKi: 5.9 |
+
5-HT7, pKi: 6.3 |
95% | ||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| Concentration | Treated Time | Description | References | |
| MDCK-II-BCRP cells | 0.2, 1, 10 µM | 1 hour | Evaluate the inhibitory effects of Sarpogrelate and M-1 on BCRP-mediated prazosin transport, showing no significant inhibition | Drug Des Devel Ther. 2016 Sep 14;10:2959-2972 |
| MDCK-II-P-gp cells | 0.2, 1, 10 µM | 1 hour | Evaluate the inhibitory effects of Sarpogrelate and M-1 on P-gp-mediated loperamide transport, showing <10% inhibition | Drug Des Devel Ther. 2016 Sep 14;10:2959-2972 |
| Cardiomyocytes | 1 µM | 48 hours | Suppressed cardiomyocyte hypertrophy induced by PE, Ang II, and ET-1 | Pharmaceuticals (Basel). 2021 Dec 5;14(12):1268 |
| Administration | Dosage | Frequency | Description | References | ||
| Albino BALBc/J mice | Light-induced retinopathy model | Intraperitoneal injection | 25 mg/kg | Single dose, lasting 1 hour | To investigate the neuroprotective effects and mechanisms of Sarpogrelate in a light-induced retinopathy model. Results showed that Sarpogrelate exerts neuroprotection through transient activation of the MAPK/ERK pathway and sustained activation of CREB, leading to transcription of anti-apoptotic genes Bcl2, Xiap, and Ucp3. | Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):462-471 |
| C57BL/6J male mice | Transverse aortic constriction (TAC) surgery-induced heart failure model | Oral | 5 mg/kg | Once daily for 8 weeks | Suppressed TAC-induced cardiac hypertrophy and systolic dysfunction | Pharmaceuticals (Basel). 2021 Dec 5;14(12):1268 |
| New Zealand white rabbits | High cholesterol diet-induced atherosclerosis model | Oral | 5 mg/kg/day | Once daily for 90 days | To investigate the effects of SP on high cholesterol diet-induced atherosclerosis. Results showed that SP reduced plasma cholesterol and triglyceride levels, decreased oxidative stress and blood viscosity, and inhibited the formation of atherosclerotic plaques. | J Cell Mol Med. 2012 Oct;16(10):2394-400 |
| BALB/c mice | Light-induced retinopathy model | Intraperitoneal injection | 5, 15, 30, 40, 50 mg/kg | 48, 24, and 0 hours before and 24 and 48 hours after exposure | To evaluate the protective effect of sarpogrelate on light-induced retinopathy. Results showed that a 50 mg/kg dose completely protected retinal morphology and function. | Invest Ophthalmol Vis Sci. 2015 Jul;56(8):4560-9 |
| 计算器 | ||||
| 存储液制备 | ![]() |
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 |
|
| CAS号 | 135159-51-2 |
| 分子式 | C24H32ClNO6 |
| 分子量 | 465.97 |
| SMILES Code | O=C(OC(COC1=CC=CC=C1CCC2=CC=CC(OC)=C2)CN(C)C)CCC(O)=O.[H]Cl |
| MDL No. | MFCD00887582 |
| 别名 | MCI-9042; Sarpogrelate (hydrochloride); Sarpogrelate hydrochloride |
| 运输 | 蓝冰 |
| InChI Key | POQBIDFFYCYHOB-UHFFFAOYSA-N |
| Pubchem ID | 444005 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, 2-8°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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