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

Tesaglitazar 是一種過(guò)氧物酶體 PPAR alpha/gamma 受體的雙重激動(dòng)劑，對(duì) PPARγ 的作用比 PPARα 強(qiáng)，對(duì)大鼠和人類 PPARα 作用的 EC50 分別為 13.4 μM 和 3.6 μM，對(duì)大鼠和人類 PPARγ 作用的 EC50 為 0.2 μM。Tesaglitazar 在大鼠皮下組織中，誘導(dǎo)間質(zhì)間充質(zhì)細(xì)胞 DNA 合成和纖維肉瘤形成。

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Tesaglitazar Chemical Structure

Tesaglitazar Chemical Structure

CAS No. : 251565-85-2

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥809
In-stock
1 mg ￥500
In-stock
5 mg ￥900
In-stock
10 mg ￥1350
In-stock
50 mg ￥4250
In-stock
100 mg ￥5950
In-stock
200 mg   詢價(jià)  
500 mg   詢價(jià)  

* Please select Quantity before adding items.

Customer Review

查看 PPAR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats[1].

IC50 & Target

EC50: 13.4 μM (rat PPARα), 3.6 μM (human PPARα), 0.2 μM (PPARγ)[1]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
CV-1 EC50
0.704 μM
Compound: (S)-tesaglitazar
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
3.124 μM
Compound: (S)-tesaglitazar
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 EC50
0.36 μM
Compound: (S)-2b
Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
[PMID: 28539218]
HEK293 EC50
3.8 μM
Compound: (S)-2b
Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
[PMID: 28539218]
HepG2 EC50
0.013 μM
Compound: tesaglitazar
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
[PMID: 18805005]
HepG2 EC50
0.82 μM
Compound: tesaglitazar
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
[PMID: 18805005]
HepG2 EC50
3528 nM
Compound: 3,tesaglitazar
Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay
[PMID: 17157019]
HepG2 EC50
9798 nM
Compound: 3,tesaglitazar
Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
[PMID: 17157019]
Clinical Trial
分子量

408.47

Formula

C20H24O7S
CAS 號(hào)
性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 200 mg/mL (489.63 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.4482 mL 12.2408 mL 24.4816 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)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(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.18%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4482 mL 12.2408 mL 24.4816 mL 61.2040 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 mL 12.2408 mL
10 mM 0.2448 mL 1.2241 mL 2.4482 mL 6.1204 mL
15 mM 0.1632 mL 0.8161 mL 1.6321 mL 4.0803 mL
20 mM 0.1224 mL 0.6120 mL 1.2241 mL 3.0602 mL
25 mM 0.0979 mL 0.4896 mL 0.9793 mL 2.4482 mL
30 mM 0.0816 mL 0.4080 mL 0.8161 mL 2.0401 mL
40 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5301 mL
50 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
60 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0201 mL
80 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7651 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 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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Inquiry Information

產(chǎn)品名稱：
Tesaglitazar
目錄號(hào)：
HY-17444
需求量：