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Cilostazol

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Chemical Structure| 73963-72-1 同义名 : OPC 13013;OPC 21;Cilostazolum;Cilostazole;Pletal;Pletaal
CAS号 : 73963-72-1
货号 : A506538
分子式 : C20H27N5O2
纯度 : 98%
分子量 : 369.461
MDL号 : -
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(135.33 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • PDE3

    PDE3, IC50:0.2 μM
描述 Type 3 cyclic nucleotide phosphodiesterase (PDE-3) isoforms exhibit a high affinity ("low K(m)") for cAMP and are specifically inhibited by cGMP and a number of pharmacological agents. The PDE-3 family consists of at least two isozymes, PDE-3A (cardiac type) and PDE-3B (adipocyte type), with distinct tissue-specific distributions[3]. Cilostazol is a 2-oxo-quinoline derivative with antithrombotic, vasodilator, antimitogenic and cardiotonic properties. The compound is a potent inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system (IC50: 0.2 μM). There is no relevant effect by cilostazol on PDE 1, 2 and 4 at comparable concentrations, and only a minor effect on PDE 5 (IC50: 5 ± 8 mM). In addition, there was inhibition of adenosine uptake, eventually resulting in changes in cAMP levels[4]. In vitro, cilostazol inhibited adenosine uptake into cardiac myocytes, coronary artery smooth muscle cells and endothelial cells, with a median effective concentration of 10 μM, which might result from stimulation of adenosine A1 receptors and might counteract the increase of cAMP via PDE-inhibition[4]. Cilostazol inhibits platelet aggregation and has considerable antithrombotic effects in vivo. The compound relaxed vascular smooth muscle and inhibited mitogenesis and migration of vascular smooth muscle cells and decreaseed levels of serum triglycerides and caused some increase in HDL-cholesterol levels[4]. In the rat carotid injury model, single local application of cilostazol resulted in a marked inhibition of intima proliferation. Interestingly, the tissue concentration of cilostazol in the carotid artery and muscle around the carotid artery was considerably higher than in plasma, which was probably related to its highly lipophilic nature. There was also suppression of neointimal formation in dog grafted veins, which appeared to be related to inhibition of angiotensin II forming enzymes[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL
参考文献

[1]Liu Y, Shakur Y, et al. Cilostazol (pletal): a dual inhibitor of cyclic nucleotide phosphodiesterase type 3 and adenosine uptake. Cardiovasc Drug Rev. 2001 Winter;19(4):369-86.

[2]Cone J, Wang S, et al. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504.

[3]Nagaoka T, Shirakawa T, Kasuya J, Balon TW, Manganiello VC, Fujita-Yamaguchi Y. Cyclic nucleotide PDE-3. Quantitation of PDE-3A and -3B mRNAs in rat tissues by RNase protection assay. Cell Biochem Biophys. 1998;29(1-2):49-66. doi: 10.1007/BF02737828. PMID: 9631238.

[4]Schrör K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. doi: 10.1046/j.1463-1326.2002.0040s2s14.x. PMID: 12180353.