| CAS NO: | 135159-51-2 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| Cas No. | 135159-51-2 |
| 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 | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Ki: 8.39 nM Sarpogrelate (MCI-9042) was shown to have the same affinity as ritanserin for 5-HT2A receptors, [1]. The blockade of 5-HT2A receptors can inhibit thrombus formation suppresses platelet aggregation and inhibits vascular smooth muscle cell proliferation [2]. In vitro: The major metabolite (R,S)-M-1, and M-1 enantiomers of sarpogrelate specifically blocked 5-HT at 5-HT2A receptors. The stereochemical configuration of the ligands does not obviously play a key role at binding to the 5-HT2A receptor [2]. In vivo: PAD patients were divided into two groups. One group treated with 100 mg sarpogrelate in oral 3 times one day for 12 weeks (n = 10), while the other group who remained on conventional therapy as control group (n = 11). Forearm blood flow (FBF) and leg blood flow (LBF) responses to reactive hyperemia (RH) and sublingual administration of nitroglycerin (NTG) were measured by strain-gauge plethysmography. After twelve weeks of its administration, FBF and LBF responses during RH exhibited significant increases from 13.2 6 1.7 to 18.1 6 2.2 mL/min every 100 mL tissue (P , 0.01) and from 8.2 6 0.9 to 14.2 6 2.1 mL/min every 100 mL tissue (P , 0.05), respectively. Augmentation of FBF and LBF induced by sarpogrelate responses to RH was maintained at 24 weeks. The control group had no change observed in at each follow-up time point. The changes in FBF and LBF after sublingual NTG were similar during follow-up periods in the two groups. These findings suggest that longterm oral administration of sarpogrelate improves vascular function in patients with PAD [3]. Clinical trial: Clinical study has been conducted. References: |
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