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

BMS-687453 是一種有效的，選擇性的 PPARα 激動劑，對人 PPARα 的 EC50 和 IC50 分別為 10 nM 和 260 nM；較弱地抑制 PPARγ 的活性，EC50 和 IC50 值分別為 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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規(guī)格 價格 是否有貨 數量
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
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100 mg 現貨 詢價
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

查看 PPAR 亞型特異性產品:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產品資料

  • 參考文獻

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)

細胞效力
(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]
體外研究
(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.
體內研究
(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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數據
細胞實驗： 

DMSO 中的溶解度 : ≥ 100 mg/mL (224.79 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質量 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
查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據您的 實驗動物和給藥方式 選擇適當的溶解方案。

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.62 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (5.62 mM); 懸濁液; 超聲助溶

    此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網站選購。 ，Tween 80，均可在 MCE 網站選購。
計算結果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯系。
動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產品資料
參考文獻
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.
參考文獻

完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

可選溶劑 濃度 溶劑體積 質量 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.

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BMS-687453
目錄號：
HY-10678
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