Tesaglitazar

Name: Tesaglitazar
Brand: MedChemExpress
SKU: HY-17444
Rating: 4.5 (1 reviews)

Cat. No.: HY-17444 Purity: 99.18%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

Tesaglitazar is a dual-target PPARα/γ agonist with an EC₅₀ of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain.

For research use only. We do not sell to patients.

Tesaglitazar Chemical Structure

CAS No. : 251565-85-2

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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10 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Purity & Documentation
References
Customer Review

Description

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]

In Vitro

Tesaglitazar mediates PPAR_α transcriptional activation with EC₅₀ of 13.4 μM and 3.6 μM for rat and human PPAR_α, respectively, and EC₅₀ of approximately 0.2 μM for rat and human PPAR_γ[1].
Tesaglitazar (2 μM; 6 hours pretreatment) significantly inhibited 10 μM Capsaicin (HY-10448)-induced cobalt influx into dorsal root ganglion (DRG) neurons in a cobalt uptake assay, and this inhibitory effect was PPAR_α- and PPAR_γ-dependent^[3].

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

In Vivo

Tesaglitazar (0.3-10 μmol/kg; po; once daily; 104 weeks) induces subcutaneous stromal sarcomas (fibrosarcomas) in Wistar Hannover Galas rats, and also induces a variety of non-neoplastic changes, such as cardiac hypertrophy and liver changes^[1].
Tesaglitazar (1, 10 μmol/kg; po; once daily; 2 or 12 weeks) in Wistar Hannover Galas rats, sustained stimulation of DNA synthesis, increased BrdU-labeled cells^[1].
Tesaglitazar (50 nmol/kg; sc; once daily; 14 days) reduced body weight, food intake, fasting blood glucose and insulin levels, improved insulin sensitivity and glucose metabolism, and had no significant effect on renal function in the male C57BL/6J diet-induced obesity (DIO) mouse model^[2].
Tesaglitazar (5 or 100 nmol/kg; sc; single dose) induced an acute deterioration in glucose tolerance at a high dose (100 nmol/kg), but a low dose (5 nmol/kg) reduced body weight, food intake and fasting blood glucose levels and improved glucose tolerance^[2] in the DIO mouse model^[2].
Tesaglitazar (10-20 μg/kg; intraperitoneal injection; single dose) significantly restored the mechanical paw withdrawal threshold (PWT) in the Streptozotocin (HY-13753)-induced diabetic neuropathy pain model in rats without affecting blood glucose levels^[3].

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

Animal Model:	Wistar Hannover Galas rats (6-8 weeks old; carcinogenicity model)^[1]
Dosage:	0.3, 1, 3, 10 μmol/kg (dissolved in 5mM sodium hydrogen carbonate buffer solution, pH 8.5)
Administration:	Oral gavage, once daily, 104 weeks
Result:	Induced subcutaneous mesenchymal sarcomas (fibrosarcomas) in both male and female rats (10 μmol/kg). Caused various non-neoplastic changes, such as myocardial hypertrophy, liver changes, and alterations in multiple organ systems.

Clinical Trial

Molecular Weight

408.47

Formula

C₂₀H₂₄O₇S

CAS No.

251565-85-2

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
10 mM	0.2448 mL	1.2241 mL	2.4482 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.18%

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Data Sheet (274 KB) SDS (392 KB)

COA (246 KB) HNMR (157 KB) RP-HPLC (246 KB) LCMS (416 KB)

Handling Instructions (2659 KB)

References

[1]. Hellmold H, et al. Tesaglitazar, a PPARalpha/gamma agonist, induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats. Toxicol Sci. 2007 Jul;98(1):63-74. [Content Brief]

[2]. Quarta C, et al. GLP-1-mediated delivery of tesaglitazar improves obesity and glucose metabolism in male mice. Nat Metab. 2022 Aug;4(8):1071-1083. [Content Brief]

[3]. Alsalem M, et al. Effects of Dual Peroxisome Proliferator-Activated Receptors α and γ Activation in Two Rat Models of Neuropathic Pain. PPAR Res. 2019 Apr 17;2019:2630232. [Content Brief]

Complete Stock Solution Preparation Table

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

Tesaglitazar Related Classifications

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:

Tesaglitazar251565-85-2PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Tesaglitazar

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