Sarpogrelate hydrochloride
(Synonyms: 盐酸沙格雷酯; MCI-9042) 目录号 : GC16202
Sarpogrelate hydrochloride是一种高选择性5-羟色胺（5-HT）2受体拮抗剂（5-HT2A: pKi = 8.52；5-HT2B: pKi = 6.57；5-HT2C: pKi = 7.43）。
Cas No.:135159-51-2
Sample solution is provided at 25 µL, 10mM.
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Sarpogrelate hydrochloride is a highly selective 5-hydroxytryptamine (5-HT) 2 receptor antagonist (5-HT2A: pKi = 8.52; 5-HT2B: pKi = 6.57; 5-HT2C: pKi = 7.43) [1]. Sarpogrelate hydrochloride inhibits serotonin-induced platelet aggregation and promotes vasodilation, improving peripheral arterial blood flow [2]. Sarpogrelate hydrochloride is primarily used to treat peripheral arterial disease associated with intermittent claudication [3-4].
In human endothelial cells, Sarpogrelate (0.1-10μM; 24h) reverses the increase in monocyte adhesion to endothelial cells under high-glucose conditions [5]. In Raw 264.7 cells, Sarpogrelate hydrochloride (20μM; 24h) treatment inhibited LPS-stimulated macrophage migration and activation [6].
In tubulointerstitial injury mice model Sarpogrelate hydrochloride (3-300mg/kg; po; 4 weeks) can improve renal dysfunction and fibrosis pathological changes [7]. In endotoxin shock rat model, Sarpogrelate hydrochloride (0-30mg/kg; iv; single injection) treatment reduces the production of proinflammatory cytokines, alleviates lung damage, and reduces the mortality rate of endotoxic shock [8].
References:
[1]. Rashid M, Manivet P, Nishio H, et al. Identification of the binding sites and selectivity of sarpogrelate, a novel 5-HT2 antagonist, to human 5-HT2A, 5-HT2B and 5-HT2C receptor subtypes by molecular modeling[J]. Life sciences, 2003, 73(2): 193-207.
[2]. Miyazaki M, Higashi Y, Goto C, et al. Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease[J]. Journal of cardiovascular pharmacology, 2007, 49(4): 221-227.
[3]. Lu Y, Li J, Xie J, et al. Effects of sarpogrelate hydrochloride on peripheral arterial disease: A meta-analysis of randomized controlled trials[J]. Medicine, 2019, 98(46): e17266.
[4]. Ma B, Fan X, Liu P. Therapeutic effects of medication use on intermittent claudication: a network meta-analysis[J]. Journal of Cardiovascular Pharmacology, 2021, 77(2): 253-262.
[5]. Su Y, Mao N, Li M, et al. Sarpogrelate inhibits the expression of ICAM-1 and monocyte–endothelial adhesion induced by high glucose in human endothelial cells[J]. Molecular and cellular biochemistry, 2013, 373(1): 195-199.
[6]. Lee E S, Lee M Y, Kwon M H, et al. Sarpogrelate hydrochloride ameliorates diabetic nephropathy associated with inhibition of macrophage activity and inflammatory reaction in db/db mice[J]. PloS one, 2017, 12(6): e0179221.
[7]. Hamasaki Y, Doi K, Maeda-Mamiya R, et al. A 5-hydroxytryptamine receptor antagonist, sarpogrelate, reduces renal tubulointerstitial fibrosis by suppressing PAI-1[J]. American Journal of Physiology-Renal Physiology, 2013, 305(12): F1796-F1803.
[8]. Nishiyama T. Acute effects of sarpogrelate, a 5-HT2A receptor antagonist on cytokine production in endotoxin shock model of rats[J]. European journal of pharmacology, 2009, 614(1-3): 122-127.
Sarpogrelate hydrochloride是一种高选择性5-羟色胺（5-HT）2受体拮抗剂（5-HT2A: pKi = 8.52；5-HT2B: pKi = 6.57；5-HT2C: pKi = 7.43） [1]。Sarpogrelate hydrochloride可抑制血清素诱导的血小板聚集，促进血管扩张，从而改善外周动脉血流 [2]。盐酸沙格雷酯主要用于治疗间歇性跛行相关的外周动脉疾病 [3-4]。
在人内皮细胞中，Sarpogrelate hydrochloride（0.1-10μM; 24h）可逆转高糖条件下单核细胞粘附于内皮细胞的增加 [5]。在Raw 264.7细胞中，Sarpogrelate hydrochloride（20μM；24h）处理可抑制LPS刺激的巨噬细胞迁移和活化 [6]。
在肾小管间质损伤小鼠模型中，Sarpogrelate hydrochloride（3-300mg/kg；po；4周）可改善肾功能障碍和纤维化病理改变 [7]。在内毒素休克大鼠模型中，Sarpogrelate hydrochloride（0-30mg/kg；iv；单次注射）治疗可减少促炎细胞因子的产生，减轻肺损伤，降低内毒素休克的死亡率 [8]。
| Cell experiment [1]: | |
Cell lines | Human endothelial cells |
Preparation Method | The study was carried out on seven groups: normal glucose control (5.5mM), Sarpogrelate hydrochloride control (5.5mM glucose plus 10.0μM Sarpogrelate hydrochloride), hyperosmolarity (5.5mM glucose plus 19.5mM mannitol), high glucose (HG, 25mM), low dose Sarpogrelate hydrochloride (25mM glucose plus 0.1μM Sarpogrelate hydrochloride), medium dose Sarpogrelate hydrochloride (25mM glucose plus 1.0μM Sarpogrelate hydrochloride) and high dose Sarpogrelate hydrochloride (25mM glucose plus 10.0μM Sarpogrelate hydrochloride). Human endothelial cells from umbilical vein (HUVEC) were incubated with normal (5.5mM) and high concentrations (25mM) of glucose for 24h. |
Reaction Conditions | 0.1-10μM; 24h |
Applications | Sarpogrelate reverses the increase in monocyte adhesion to endothelial cells under high-glucose conditions. |
| Animal experiment [2]: | |
Animal models | Tubulointerstitial injury mice model |
Preparation Method | This experiment used eight-week-old wild-type male C57BL/6 mice. Both the Sarpogrelate hydrochloride-treated group (adenine-containing diet (Ad)+Sarpogrelate hydrochloride group) and the untreated group (Ad group) were fed a diet containing 0.2% wt/wt adenine for six weeks. The Ad+Sarpogrelate hydrochloride group received Sarpogrelate hydrochloride dissolved in distilled water for four weeks, starting two weeks after the start of the adenine-containing diet. The Sarpogrelate hydrochloride solution concentration was adjusted based on the mice's drinking water intake, with daily doses of 3, 30, and 300mg/kg Sarpogrelate hydrochloride administered. The Ad group received distilled water only. The normal diet group (N group) was fed a normal diet and water for six weeks. The normal diet was purchased from Oriental Yeast. Its composition, except for adenine, was identical to the adenine-containing diet. After the start of the adenine diet, body weight was measured and blood samples were collected every two weeks. |
Dosage form | 3-300mg/kg; po; 4 weeks |
Applications | Sarpogrelate hydrochloride can improve renal dysfunction and fibrosis pathological changes in model mice. |
References: | |
| Cas No. | 135159-51-2 | SDF | |
| 别名 | 盐酸沙格雷酯; MCI-9042 | ||
| Canonical SMILES | O=C(CCC(O)=O)OC(CN(C)C)COC1=CC=CC=C1CCC2=CC(OC)=CC=C2.Cl | ||
| 分子式 | C24H32ClNO6 | 分子量 | 465.97 |
| 溶解度 | ≥ 23.3mg/mL in DMSO | 储存条件 | Store at 2-8°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1461 mL | 10.7303 mL | 21.4606 mL |
| 5 mM | 0.4292 mL | 2.1461 mL | 4.2921 mL |
| 10 mM | 0.2146 mL | 1.073 mL | 2.1461 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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