Cilostazol
(Synonyms: 西洛他唑; OPC 13013) 目录号 : GC15890A PDE3A inhibitor
Cas No.:73963-72-1
Sample solution is provided at 25 µL, 10mM.
Cilostazol is specific inhibition of cyclic nucleotide phosphodiesterase 3 (PDE3) with IC50 value of 200 nM.[1]
PDE3 is one of phosphodiesterase. PDE3 plays an important role in regulating vascular smooth muscle, heart muscle and platelet aggregation, so, it is clinically significant. The PDE3 family consists of two members including PDE3A and PDE3B. PDE3A is mainly related cardiovascular function and PDE3B is mainly related to lipolysis. The activity of PDE3 is regulated by phosphorylation pathways. PDE 3 is activited via phosphorylation at different phosphorylation sites by protein kinase A and protein kinase B. PDE3 enzymes also are involved in regulation of vascular and cardiac smooth muscle contractility.
Cilostazol prevents platelet aggregation by specifically and selectively inhibiting PDE3 in platelets with IC50 value of 200 nM. Cilostazol also cause intracellular cAMP levels increasing by inhibiting adenosine uptake leading to increased adenosine levels in cells. Cilostazol also inhibits the expression of platelet surface P-selectin, platelet factor 4 (PF4), thromboxane B2 production release. Cilostazol also cause decrease in triglyceride levels and an increase in high-density lipoprotein. [1]
Cilostazol may has effective function in dementia. Cilostazol has beneficial effects on learning impairment induced by Aβ25-35 in mice. Cilostazol attenuated the impairment induced by Aβ25-35 at 100 mg/kg.[2]
References:
[1]. Rondina MT, Weyrich AS: Targeting phosphodiesterases in anti-platelet therapy. Handb Exp Pharmacol 2012(210):225-238.
[2]. Hiramatsu M, Takiguchi O, Nishiyama A, Mori H: Cilostazol prevents amyloid beta peptide(25-35)-induced memory impairment and oxidative stress in mice. Br J Pharmacol 2010, 161(8):1899-1912.
Cas No. | 73963-72-1 | SDF | |
别名 | 西洛他唑; OPC 13013 | ||
化学名 | 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one | ||
Canonical SMILES | C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4 | ||
分子式 | C20H27N5O2 | 分子量 | 369.46 |
溶解度 | ≥ 15.4 mg/mL in DMSO, ≥ 3.95 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
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