1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. PPAR
  3. Pirinixic acid

Pirinixic acid  (Synonyms: 匹立尼酸; Wy-14643)

目录号: HY-16995 纯度: 99.80%
COA 产品使用指南

Pirinixic acid (Wy-14643) 是一种有效的 PPARα 激动剂,对鼠的 PPARαPPARγEC50 值分别为 0.63 μM, 32 μM,对人的 PPARαPPARγPPARδEC50 值分别为 5.0 μM,60 μM,35 μM。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Pirinixic acid Chemical Structure

Pirinixic acid Chemical Structure

CAS No. : 50892-23-4

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
In-stock
1 mg ¥156
In-stock
5 mg ¥312
In-stock
10 mg ¥500
In-stock
50 mg ¥780
In-stock
100 mg ¥1100
In-stock
250 mg ¥2450
In-stock
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

查看 PPAR 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

IC50 & Target[1]

PPARα

0.63 μM (EC50)

PPARγ

32 μM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
COS-7 IC50
36.3 μM
Compound: 1
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
[PMID: 25037914]
COS-7 EC50
39.8 μM
Compound: 1, WY-14,643
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
[PMID: 25022880]
COS-7 EC50
53.7 μM
Compound: 1, WY-14,643
Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
[PMID: 25022880]
COS-7 EC50
53.7 μM
Compound: 1
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
[PMID: 20307981]
COS-7 IC50
53.7 μM
Compound: 1
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
[PMID: 25037914]
CV-1 EC50
0.13 μM
Compound: Wy14643
Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay
Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay
[PMID: 22579420]
HEK293 EC50
23.33 μM
Compound: WY-14643
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
[PMID: 23265844]
HepG2 EC50
0.04 μM
Compound: WY-14643
Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
[PMID: 19053776]
HepG2 EC50
1.56 μM
Compound: Wy 14,643
Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
[PMID: 23171045]
HepG2 EC50
1.56 μM
Compound: Wy-14,643
Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay
Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay
[PMID: 25462281]
HepG2 EC50
1.6 μM
Compound: Wy-14,643
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
[PMID: 22341573]
HepG2 EC50
1.6 μM
Compound: WY-14643
Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
[PMID: 22081932]
HepG2 EC50
1.6 μM
Compound: WY-14643
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
[PMID: 19775169]
HepG2 EC50
1.6 μM
Compound: WY-14643
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
[PMID: 18835719]
HepG2 EC50
1.62 μM
Compound: Wy-14,643
Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
[PMID: 25497132]
HepG2 EC50
1.62 μM
Compound: WY-14643
Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
[PMID: 19053776]
HepG2 EC50
3.46 μM
Compound: WY14643
Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay
Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay
[PMID: 23502212]
HepG2 EC50
4.8 μM
Compound: WY-14643
Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
[PMID: 18625559]
HepG2 EC50
4800 nM
Compound: WY-14643
Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
[PMID: 21450468]
HepG2 EC50
7.1 μM
Compound: WY14643
Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
[PMID: 23502212]
MCF7 EC50
542 nM
Compound: WY-14643
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay
[PMID: 24936232]
MCF7 EC50
650 nM
Compound: WY-14643
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay
[PMID: 24936232]
U2OS EC50
12 μM
Compound: WY-14643
Agonist activity at human PPARalpha in U2OS cells by transactivation assay
Agonist activity at human PPARalpha in U2OS cells by transactivation assay
[PMID: 18329751]
体外研究
(In Vitro)

Pirinixic acid (Wy-14643) 是 PPARα 的激动剂,小鼠 PPARαPPARγ 的 EC50 为 0.63 μM,32 μM,人 PPARα,PPARγ 为 5.0 μM,60 μM,35 μM和 PPARδ[1]
Pirinixic acid (Wy-14643;0,10,100 μM) 增强滑膜成纤维细胞中 PPAR-α 的蛋白表达。Pirinixic acid (0,10,100 μM) 对 LPS 刺激的滑膜成纤维细胞中的 NO 和 PGE2 产生有抑制作用。Pirinixic acid 还有效下调滑膜成纤维细胞中炎症介质如 VCAM-1、ICAM-1、ET-1 和 TF 的表达,阻断滑膜成纤维细胞中 LPS 诱导的 NF-kB 活化、IkB 磷酸化和 NF-kB 核转位,但 Pirinixic acid 对 PPAR-α 沉默的细胞没有影响[2]

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

体内研究
(In Vivo)

Pirinixic acid (Wy-14643;10 mg/kg,iv) 降低肥胖大鼠的肝损伤和脂质过氧化 (MDA) 水平。Pirinixic acid 还会导致 Sham 和缺血再灌注 (IR) 组的 SIRT1 活性增加,但对 SIRT3 蛋白表达没有影响。Pirinixic acid 可提高大鼠的 NAD+ 和 ATP 水平,并防止内质网应激 (ERS)[3]

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

分子量

323.80

Formula

C14H14ClN3O2S

CAS 号
性状

固体

颜色

White to off-white

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 (308.83 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)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0883 mL 15.4416 mL 30.8833 mL
5 mM 0.6177 mL 3.0883 mL 6.1767 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: 10 mg/mL (30.88 mM); 悬浊液; 超声助溶

    此方案可获得 10 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    1 mL 工作液为例,取 100 μL 100.0 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: ≥ 2.08 mg/mL (6.42 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 20.8 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

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: 99.80%

参考文献
Cell Assay
[2]

Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Pirinixic acid. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Pirinixic acid. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve[2].

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

Animal Administration
[2]

Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Wy-14643. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Wy-14643. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve[2].

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

参考文献

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 3.0883 mL 15.4416 mL 30.8833 mL 77.2082 mL
5 mM 0.6177 mL 3.0883 mL 6.1767 mL 15.4416 mL
10 mM 0.3088 mL 1.5442 mL 3.0883 mL 7.7208 mL
15 mM 0.2059 mL 1.0294 mL 2.0589 mL 5.1472 mL
20 mM 0.1544 mL 0.7721 mL 1.5442 mL 3.8604 mL
25 mM 0.1235 mL 0.6177 mL 1.2353 mL 3.0883 mL
30 mM 0.1029 mL 0.5147 mL 1.0294 mL 2.5736 mL
40 mM 0.0772 mL 0.3860 mL 0.7721 mL 1.9302 mL
50 mM 0.0618 mL 0.3088 mL 0.6177 mL 1.5442 mL
60 mM 0.0515 mL 0.2574 mL 0.5147 mL 1.2868 mL
80 mM 0.0386 mL 0.1930 mL 0.3860 mL 0.9651 mL
100 mM 0.0309 mL 0.1544 mL 0.3088 mL 0.7721 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.

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
Pirinixic acid
目录号:
HY-16995
需求量: