Sarpogrelate hydrochloride (MCI-9042) 是一种选择性的5-HT2R拮抗剂，对 5-HT2A，5-HT2B，和 5-HT2C受体的pKi值分别为 8.52、6.57 和 7.43。Sarpogrelate hydrochloride 对 5-HT1，5-HT3，5-HT4，α1-，α2- 和 β-肾上腺素受体，组胺 H1，H2以及毒蕈碱 M3受体缺乏显著的拮抗活性。Sarpogrelate hydrochloride 可用于研究与血栓形成有关的血管疾病。
| 生物活性 | Sarpogrelate hydrochloride (MCI-9042) is a selective5-HT2Rantagonist, withpKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2Creceptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2and muscarinic M3receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3]. |
| IC50& Target[1] | 5-HT2AReceptor 8.52 (pKi) | 5-HT2BReceptor 6.57 (pKi) | 5-HT2CReceptor 7.43 (pKi) |
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体外研究
(In Vitro) | Sarpogrelate is selective for 5-HT2(pKi=7.54) over 5-HT1(pKi=4.58), α1-, α2-, and β-adrenergic (pKi=3.17-6.19), and muscarinic receptors (pKi=4.39)[2].
Sarpogrelate (10 μM) significantly reduces the number of platelet-rich plasma (PRP)-induced THP-1 cell that adheres to human umbilical vein endothelial cells (HUVECs)[3].
Sarpogrelate (10 μM) significantly reduces the expression of PRP-induced E-selectin in HUVECs[3].
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体内研究
(In Vivo) | Sarpogrelate (5 mg/kg; i.p. daily for 4 weeks) inhibits HFFD-induced obesity and decreases leukocyte-endothelial interactions in mice[3].
| Animal Model: | Male C57BL/6 mice (7 weeks old) are fed normal chow (NC) or a high-fat diet with 30% fructose in the drinking water (HFFD)[3] | | Dosage: | 5 mg/kg | | Administration: | I.p. daily for 4 weeks | | Result: | Prevented the HFFD-induced increases of the body weight, visceral fat weight, and serum monocyte chemoattractant protein-1 levels.
Decreased leukocyte-endothelial interactions and serum monocyte chemoattractant protein-1 (MCP-1) level. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 62 mg/mL(133.06 mM) H2O : 33.33 mg/mL(71.53 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 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 | 1.0730 mL | 2.1461 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： PBS Solubility: 10 mg/mL (21.46 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.37 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.37 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.37 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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