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Ciprofibrate

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Chemical Structure| 52214-84-3 同义名 : Win35833;WIN 35,833;CCRIS 173;BRN 1984981;(±)-Ciprofibrate
CAS号 : 52214-84-3
货号 : A240639
分子式 : C13H14Cl2O3
纯度 : 98%
分子量 : 289.15
MDL号 : MFCD00467135
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(363.13 mM)，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
描述 Ciprofibrate is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate (500 μM; 4 hours) increases the PPARa phosphorylation level in rat Fao cells[3]. In a LucLite assay, Ciprofibrate (10-100μM; 24 hours) induces PPARR activation by existing increased LUC activities in the rat liver H4IIEC3 cells transfected with PPRE-AB LUC reporter gene plasmid[4]. A single dose of ciprofibrate (5 mg/kg by gastric intubation) significantly induces rat liver bilirubin conjugation as well as UGT1A1, UGT1A5 and PPARαexpression[5]. The main effects of ciprofibrate on G cells are mediated from the antrum lumen, and the mechanism is dependent on PPAR-alpha[6]. Ciprofibrate inhibited cigarette smoke extract-induced rat ASM cell contraction and proliferation in vitro. Ciprofibrate improved pulmonary function, inhibited airway hypercontraction, and ameliorated morphological small airway remodeling, including airway smooth muscle proliferation, in CS-exposed rats. Ciprofibrate also significantly reduced IL-1β, IL-12p70, IL-17A and IL-18 expression, which are related to airway remodeling, in the sera of CS-exposed rats[7].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03031821 Prostate Cancer ... 展开 >> Metabolic Syndrome 收起 << Phase 3 Not yet recruiting June 1, 2023 Canada, British Columbia ... 展开 >> BC Cancer Agency - Vancouver Cancer Centre Not yet recruiting Vancouver, British Columbia, Canada, V5Z 4E6 Contact: Bernie Eigl, MD    604-877-6000    bernie.eigl@bccancer.bc.ca    Principal Investigator: Bernie Eigl, MD 收起 <<
NCT01480687 Hypertension ... 展开 >>Hypertriglyceridemia 收起 << Phase 4 Unknown December 2012 Brazil ... 展开 >> Hospital Universitario Pedro Ernesto Recruiting Rio de Janeiro, RJ, Rio de Janeiro, Brazil Contact: Marcela A Casanova, MSc    55-21-2868-8484    cela.abreu@gmail.com 收起 <<
NCT00350038 Hypertension ... 展开 >>Dyslipidemia 收起 << Phase 4 Completed - Hungary ... 展开 >> Sanofi-aventis Budapest, Hungary 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.46mL

0.69mL

0.35mL

17.29mL

3.46mL

1.73mL

34.58mL

6.92mL

3.46mL
参考文献

[1]Clemencet MC, Muzio G, et al. Differences in cell proliferation in rodent and human hepatic derived cell lines exposed to ciprofibrate. Cancer Lett. 2005 May 26;222(2):217-26.

[2]Passilly P, Schohn H, Jannin B, Cherkaoui Malki M, Boscoboinik D, Dauca M, Latruffe N. Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate. Biochem Pharmacol. 1999 Sep 15;58(6):1001-8.

[3]Passilly P, Schohn H, Jannin B, Cherkaoui Malki M, Boscoboinik D, Dauça M, Latruffe N. Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate. Biochem Pharmacol. 1999 Sep 15;58(6):1001-8

[4]Rimando AM, Nagmani R, Feller DR, Yokoyama W. Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters. J Agric Food Chem. 2005 May 4;53(9):3403-7

[5]Heydel JM, Garnier P, Faure P, Artur Y. Ciprofibrate regulation of rat hepatic bilirubin glucuronidation and UDP-glucuronosyltransferases expression. Eur J Drug Metab Pharmacokinet. 2012 Dec;37(4):233-40

[6]Martinsen TC, Bakke I, Chen D, Sandvik AK, Zahlsen K, Aamo T, Waldum HL. Ciprofibrate stimulates the gastrin-producing cell by acting luminally on antral PPAR-alpha. Am J Physiol Gastrointest Liver Physiol. 2005 Dec;289(6):G1052-60

[7]Ke Q, Yang L, Cui Q, Diao W, Zhang Y, Xu M, He B. Ciprofibrate attenuates airway remodeling in cigarette smoke-exposed rats. Respir Physiol Neurobiol. 2020 Jan;271:103290