2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. BMS-687453

BMS-687453 是一种有效的，选择性的 PPARα 激动剂，对人 PPARα 的 EC50 和 IC50 分别为 10 nM 和 260 nM；较弱地抑制 PPARγ 的活性，EC50 和 IC50 值分别为 4100 nM 和 >15000 nM。

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BMS-687453 Chemical Structure

BMS-687453 Chemical Structure

CAS No. : 1000998-59-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1210
In-stock
1 mg ￥400
In-stock
5 mg ￥990
In-stock
10 mg ￥1580
In-stock
25 mg ￥3150
In-stock
50 mg ￥4880
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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BMS-687453 相关抗体

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.

IC50 & Target

PPARα

260 nM (IC50, Human PPARα)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 EC50
10 nM
Compound: 2, BMS-687453
Agonist activity at human PPARalpha LBD (167-468) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
Agonist activity at human PPARalpha LBD (167-468) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
[PMID: 20218621]
HEK293 EC50
4017 nM
Compound: 1
Agonist activity against human Gal4-fussed PPARgamma in HEK293 cells by luciferase reporter gene assay
Agonist activity against human Gal4-fussed PPARgamma in HEK293 cells by luciferase reporter gene assay
[PMID: 20356736]
HEK293 EC50
4100 nM
Compound: 2, BMS-687453
Agonist activity at human PPARgamma LBD (176-477) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
Agonist activity at human PPARgamma LBD (176-477) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
[PMID: 20218621]
HEK293 EC50
426 nM
Compound: 2, BMS-687453
Agonist activity at mouse PPARalpha LBD (167-469) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
Agonist activity at mouse PPARalpha LBD (167-469) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
[PMID: 20218621]
HEK293 EC50
488 nM
Compound: 2, BMS-687453
Agonist activity at syrian golden hamster PPARalpha LBD (167-468) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
Agonist activity at syrian golden hamster PPARalpha LBD (167-468) expressed in HEK293 cells coexpressing GAL4-DBD by transactivation assay
[PMID: 20218621]
HEK293 EC50
9.6 nM
Compound: 1
Agonist activity against human Gal4-fussed PPARalpha in HEK293 cells by luciferase reporter gene assay
Agonist activity against human Gal4-fussed PPARalpha in HEK293 cells by luciferase reporter gene assay
[PMID: 20356736]
HepG2 EC50
2400 nM
Compound: 2, BMS-687453
Agonist activity at full length human PPARgamma expressed in HepG2 cells co-transfected with pBL-tk-luciferase by luciferase reporter gene assay
Agonist activity at full length human PPARgamma expressed in HepG2 cells co-transfected with pBL-tk-luciferase by luciferase reporter gene assay
[PMID: 20218621]
HepG2 EC50
47 nM
Compound: 2, BMS-687453
Agonist activity at full length human PPARalpha expressed in HepG2 cells co-transfected with pBL-tk-luciferase by luciferase reporter gene assay
Agonist activity at full length human PPARalpha expressed in HepG2 cells co-transfected with pBL-tk-luciferase by luciferase reporter gene assay
[PMID: 20218621]
体外研究
(In Vitro)

BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and ∼410-fold and more than 57-fold selectivity vs human PPARγ of 4100 nM and >15000 nM in PPAR-GAL4 transactivation assays. BMS-687453 exhibits high PPARα potency (EC50 = 47 nM) with ∼50-fold selectivity vs PPARγ (EC50 = 2400 nM) in HepG2 cells. However, BMS-687453 shows less potent activities in rodent PPARα functional assays, with a moderate EC50 of 426 nM for mouse and 488 nM for hamster but remains a full PPARα agonist in both species[1].

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

BMS-687453 相关抗体:
体内研究
(In Vivo)

BMS-687453 (10, 50, 100, p.o.) dose-dependently increases serum ApoA1 protein levels and low-density lipoprotein-cholesterol (LDLc) levels in mice. BMS-687453 (1, 3, 10 mg/kg, p.o.) decreases HDLc levels in high fat-fed hamsters[1]. BMS-687453 induces PDK4 mRNA in the liver, with ED50 value of 0.24 mg/kg[2]. BMS-687453 (300 mg/kg, p.o.) causes skeletal myofiber degeneration and necrosis characterized by observed discoid changes, myofibril lysis, hyalinization, and cellular infiltration in male rats. BMS-687453 (300 mg/kg, p.o.) induces a mild toxicity in both fast and slow-twitch muscles in male rats[3].

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

444.86

Formula

C22H21ClN2O6
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 (224.79 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2479 mL 11.2395 mL 22.4790 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 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 (5.62 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 (5.62 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    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
参考文献
Kinase Assay
[1]

A homogeneous, fluorescent polarization PPARα and PPARγ binding assay is used as the primary screen for determining the PPARα and PPARγ binding affinity of compounds. The human functional activity of PPARα and PPARγ agonists is determined by using the GAL4-LBD assays. The in vitro hamster, rat, and mouse PPARα functional activities are tested in the chimeric GAL4/PPARα assay format. The data are reported as an EC50 value calculated using XLfit 4 parameter fit and floating all parameters. Full length human PPARα and PPARγ co-transfection assays in HepG2 cells are employed for further testing the leading compounds (BMS-687453)[1].

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

Male 6−8 week old human apoA1 transgenic mice are randomly assigned into different treatment groups and weighed and dosed by oral gavage (5 mL/kg body weight) once a day in the morning with vehicle alone or with compound (BMS-687453) and allowed free access to food and water. The study duration is 10 days. After dosing on day 10, mice are fasted for 4 h and sacrificed by CO2 asphyxiation, and blood samples are collected in serum-separating tubes via cardiac puncture for lipid measurements. Livers are dissected out, weighed, and quickly frozen in liquid nitrogen for future RNA analysis. Human apoA1 concentration in serum is measured using the apolipoprotein A1 kit[1].

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

BMS-687453 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 2.2479 mL 11.2395 mL 22.4790 mL 56.1975 mL
5 mM 0.4496 mL 2.2479 mL 4.4958 mL 11.2395 mL
10 mM 0.2248 mL 1.1239 mL 2.2479 mL 5.6197 mL
15 mM 0.1499 mL 0.7493 mL 1.4986 mL 3.7465 mL
20 mM 0.1124 mL 0.5620 mL 1.1239 mL 2.8099 mL
25 mM 0.0899 mL 0.4496 mL 0.8992 mL 2.2479 mL
30 mM 0.0749 mL 0.3746 mL 0.7493 mL 1.8732 mL
40 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4049 mL
50 mM 0.0450 mL 0.2248 mL 0.4496 mL 1.1239 mL
60 mM 0.0375 mL 0.1873 mL 0.3746 mL 0.9366 mL
80 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7025 mL
100 mM 0.0225 mL 0.1124 mL 0.2248 mL 0.5620 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:

BMS-6874531000998-59-3BMS687453BMS 687453PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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