生物活性分子抑制剂Cilostazol(Synonyms: 西洛他唑; OPC 13013)

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生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 Cilostazol (Synonyms: 西洛他唑; OPC 13013) 纯度: 99.91%

Cilostazol (OPC 13013) 是有效、选择性的心血管系统中磷酸二酯酶 3 亚型 PDE 3A 的抑制剂，IC50 值为 0.2 μM。

Cilostazol(Synonyms: 西洛他唑; OPC 13013)

Cilostazol Chemical Structure

CAS No. : 73963-72-1

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10 mM * 1 mL in DMSO ￥660 In-stock
50 mg ￥600 In-stock
100 mg ￥900 In-stock
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500 mg   询价  

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生物活性

Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM[1][2].

IC50 & Target

IC50: 0.2 μM ( PDE 3A)[1]
体外研究
(In Vitro)

Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of platelet aggregation induced by various agonists[2].
Cilostazol inhibits stress-induced human platelet aggregation (SIPA) dose-dependently, with an IC50 of 15 μM for SIPA, and with a similar IC50 of 12.5 μM for ADP-induced platelet aggregation[2].
Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Cilostazol (clinically used doses; p.o.; for 2 weeks) could alleviate CCl4 -induced hepatic fibrogenesis in vivo, presumably due to its direct effect to suppress HSC activation[3].
Cilostazol (intraperitoneal injection; 10 mg/kg; 7 consecutive days after ischemia) attenuates neurological dysfunctions, brain atrophy and infarct volume, and inhibits astrocyte proliferation/glial scar formation and accelerated the angiogenesis in the ischemic boundary zone 7 and 28 days after ischemia[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6J mice[3]
Dosage: 0.1% w/w, 0.3% w/w
Administration: Oral administration; fed a normal diet for 2 weeks
Result: Exhibited a lesser fibrotic area than control groups.
Animal Model: Male ICR mice[4]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 7 consecutive days after ischemia
Result: Had an effectve effects for the late injury.

Clinical Trial

分子量

369.46

Formula

C20H27N5O2
CAS 号

73963-72-1
中文名称

西洛他唑
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (135.33 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7067 mL 13.5333 mL 27.0665 mL
5 mM 0.5413 mL 2.7067 mL 5.4133 mL
10 mM 0.2707 mL 1.3533 mL 2.7067 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°C, 6 months; -20°C, 1 month。-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。

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： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (5.41 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (5.41 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (5.41 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 20.0 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9.

    [2]. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9.

    [3]. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis. Hepatol Res. 2013 Apr 19.

    [4]. Ye YL,et al. Cilostazol, a phosphodiesterase 3 inhibitor, protects mice against acute and late ischemic brain injuries.Eur J Pharmacol. 2007 Feb 14;557(1):23-31. Epub 2006 Nov 10.

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