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

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.

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Tesaglitazar Chemical Structure

Tesaglitazar Chemical Structure

CAS No. : 251565-85-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
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10 mg USD 170 In-stock
50 mg USD 600 In-stock
100 mg USD 960 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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]

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
Molecular Weight

408.47

Formula

C20H24O7S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)[C@@H](OCC)CC1=CC=C(OCCC2=CC=C(OS(=O)(C)=O)C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (489.63 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.18%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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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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Product Name:
Tesaglitazar
Cat. No.:
HY-17444
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