2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR Cytochrome P450
  4. Gemfibrozil

Gemfibrozil  (Synonyms: 吉非罗齐; CI-719)

目录号: HY-B0258 纯度: 99.88%
COA 产品使用指南

摩尔计算器

Gemfibrozil 是一种 PPAR-α 激活剂，为一种降脂剂；Gemfibrozil 同时是 P450 的非选择性抑制剂，对 CYP2C9，2C19，2C8 和 1A2 的 Ki 值分别为 5.8，24，69 和 82 μM。

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Gemfibrozil Chemical Structure

Gemfibrozil Chemical Structure

CAS No. : 25812-30-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥500
In-stock
100 mg ￥400
In-stock
500 mg ￥900
In-stock
1 g   询价  
5 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Gemfibrozil:

Gemfibrozil 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

IC50 & Target[1]

PPAR-α

 

CYP2C9

5.8 μM (Ki)

CYP2C19

24 μM (Ki)

CYP2C8

69 μM (Ki)

CYP1A2

82 μM (Ki)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BHK-21 EC50
> 100 μM
Compound: Gemfibrozil
Antiviral activity against YFV infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay
Antiviral activity against YFV infected in BHK-21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay
[PMID: 26443549]
CV-1 EC50
147.8 μM
Compound: gemfibrozil
Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs
Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs
[PMID: 17507225]
CV-1 EC50
147.8 μM
Compound: gemfibrozil
Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
[PMID: 18826205]
CV-1 EC50
193.3 μM
Compound: gemfibrozil
Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs
Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs
[PMID: 17507225]
CV-1 EC50
193.3 μM
Compound: gemfibrozil
Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
[PMID: 18826205]
HEK293 IC50
11 μM
Compound: Gemfibrozil
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate
[PMID: 22587986]
HEK293 IC50
130 μM
Compound: Gemfibrozil
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate
[PMID: 22587986]
HEK293 IC50
38 μM
Compound: Gemfibrozil
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate
[PMID: 22587986]
HEK293 EC50
59 μM
Compound: Gemfibrozil
Transactivation of human PPARalpha expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay
Transactivation of human PPARalpha expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay
10.1039/C5MD00151J
HEK293 EC50
59 μM
Compound: Gemfibrozil
Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
[PMID: 21889235]
MT4 CC50
> 100 μM
Compound: Gemfibrozil
Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT assay
Cytotoxicity against human MT4 cells assessed as cell viability after 96 hrs by MTT assay
[PMID: 26443549]
Vero 76 EC50
> 100 μM
Compound: Gemfibrozil
Antiviral activity against human CVB5 infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 3 days by plaque reduction assay
Antiviral activity against human CVB5 infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 3 days by plaque reduction assay
[PMID: 26443549]
Vero 76 CC50
> 100 μM
Compound: Gemfibrozil
Cytotoxicity against african green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by crystal violet staining method
Cytotoxicity against african green monkey Vero 76 cells assessed as cell viability after 48 to 96 hrs by crystal violet staining method
[PMID: 26443549]
Vero 76 EC50
> 100 μM
Compound: Gemfibrozil
Antiviral activity against human RSV infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by plaque reduction assay
Antiviral activity against human RSV infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity after 5 days by plaque reduction assay
[PMID: 26443549]
Vero 76 EC50
> 100 μM
Compound: Gemfibrozil
Antiviral activity against Human poliovirus 1 Sabin infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity by plaque reduction assay
Antiviral activity against Human poliovirus 1 Sabin infected in african green monkey Vero76 cells assessed as inhibition of virus-induced cytopathogenicity by plaque reduction assay
[PMID: 26443549]
体外研究
(In Vitro)

Gemfibrozil 是 PPAR-α 的激活剂，用作降脂药物[1]；也是几种 P450 亚型的非选择性抑制剂，对 CYP2C9、2C19、2C8 和 1A2 的 Ki 值分别为 5.8、24、69 和 82 μM[3]。Gemfibrozil (100，150，200 μM) 在人 U373MG 星形胶质细胞中以浓度依赖性方式抑制细胞因子诱导的 NO 产生，这种作用不是由于 iNOS mRNA 稳定性的任何变化。Gemfibrozil (50，100，200 μM) 抑制细胞因子刺激的人 U373MG 星形胶质细胞中人 iNOS 启动子衍生的荧光素酶活性。此外，Gemfibrozil (50、100、150 和 200 μM) 对细胞活力没有影响[1]。Gemfibrozil 显著抑制 M-23 和 M-1 的形成 (由 CYP2C8 和 CYP3A4 催化)，Ki (IC50) 值为 69 μM (95 μM) 和在人肝微粒体中分别为 273 μM (>250 μM)。Gemfibrozil (0-250 μM) 剂量依赖性地抑制重组体中 M-23 (IC50，68 μM) 和 M-1 (IC50，78 μM) 的形成 CYP2C8，但对重组 CYP3A4 中这些代谢物的形成没有明显影响[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Gemfibrozil 相关抗体:
体内研究
(In Vivo)

在脊髓损伤 (SCI) 前 3 天开始的 Gemfibrozil (62 mg/kg/天，口服) 处理导致运动功能下降，并诱导小鼠受伤后白质保留减少的趋势。Gemfibrozil (62 mg/kg/天，口服) 降低巨噬细胞的免疫反应性，但增加 T 细胞浸润到备用组织中[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

250.33

Formula

C15H22O3
CAS 号
性状

固体

颜色

White to off-white

中文名称

吉非罗齐
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 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (399.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.9947 mL 19.9736 mL 39.9473 mL
5 mM 0.7989 mL 3.9947 mL 7.9895 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.99 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.99 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（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 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.91%

COA (281 KB) HNMR (169 KB) LCMS (388 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[3]

Activities of CYP3A4 (testosterone 6β-hydroxylation) and CYP2C8 (paclitaxel 6α-hydroxylation) are determined. The marker substrate concentrations used, 25 μM testosterone and 1 to 5 μM paclitaxel, are comparable with or around the Km values of the reactions. Gemfibrozil is either coincubated at 37°C for 15 min with the marker substrate and NADPH (1 mM) before the reaction is initiated with human liver microsomes (0.1 mg/mL) or preincubated with human liver microsomes and NADPH for 15 min before adding the marker substrate[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[1]

Briefly, 400 μL of culture supernatant is allowed to react with 200 μL of Griess reagent and incubated at room temperature for 15 min. The optical density of the assay samples is measured spectrophotometrically at 570 nm. Fresh culture medium serves as the blank in all experiments. Nitrite concentrations are calculated from a standard curve derived from the reaction of NaNO2 in the assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice are given vehicle or gemfibrozil beginning 3 days before SCI to ensure drug availability at the time of the injury (n=5-6/group). The drug is delivered orally by dissolving it in ethanol (0.25% w/w of gemfibrozil) and coating food pellets such that each animal receives appr 62 mg/kg/day; chow for control groups is treated with ethanol. Ethanol for each group is allowed to completely evaporate before giving the food to the animals. In addition, animals receive an intraperitoneal injection of vehicle or gemfibrozil (500 µg dissolved in 200 µL PBS) 1 h after the injury, and then continued to receive the drug in their food until the end of the study (28 days post-injury)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Gemfibrozil 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9947 mL 19.9736 mL 39.9473 mL 99.8682 mL
5 mM 0.7989 mL 3.9947 mL 7.9895 mL 19.9736 mL
10 mM 0.3995 mL 1.9974 mL 3.9947 mL 9.9868 mL
15 mM 0.2663 mL 1.3316 mL 2.6632 mL 6.6579 mL
20 mM 0.1997 mL 0.9987 mL 1.9974 mL 4.9934 mL
25 mM 0.1598 mL 0.7989 mL 1.5979 mL 3.9947 mL
30 mM 0.1332 mL 0.6658 mL 1.3316 mL 3.3289 mL
40 mM 0.0999 mL 0.4993 mL 0.9987 mL 2.4967 mL
50 mM 0.0799 mL 0.3995 mL 0.7989 mL 1.9974 mL
60 mM 0.0666 mL 0.3329 mL 0.6658 mL 1.6645 mL
80 mM 0.0499 mL 0.2497 mL 0.4993 mL 1.2484 mL
100 mM 0.0399 mL 0.1997 mL 0.3995 mL 0.9987 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Gemfibrozil25812-30-0CI-719吉非罗齐CI719CI 719PPARCytochrome P450Peroxisome proliferator-activated receptorsCYPsInhibitorinhibitorinhibit

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