Sarpogrelate hydrochloride (Synonyms: MCI-9042) |
| رقم الكتالوجGC16202 |
مثبط مستقبل 5-HT2A
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| المرادفات | MCI-9042 | ||
| Canonical SMILES | O=C(CCC(O)=O)OC(CN(C)C)COC1=CC=CC=C1CCC2=CC(OC)=CC=C2.Cl | ||
| Formula | C24H32ClNO6 | M.Wt | 465.97 |
| الذوبان | ≥ 23.3mg/mL in DMSO | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1461 mL | 10.7303 mL | 21.4606 mL |
| 5 mM | 429.2 μL | 2.1461 mL | 4.2921 mL |
| 10 mM | 214.6 μL | 1.073 mL | 2.1461 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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