Reagents and instruments for immunology, cell biology and molecular biology.

Pioglitazone [111025-46-8]

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Cat# HY-13956-10mg

Size : 10mg

Brand : MedChemExpress

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Description

Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research^[2]^[3]^[4].

IC₅₀ & Target^[1]

hPPARγ

0.93 μM (EC₅₀)

mouse PPARγ

0.99 μM (EC₅₀)

hPPARδ

43 μM (EC₅₀)

hPPARα

100 μM (EC₅₀)

mouse PPARα

100 μM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.14 μM Compound: Pioglitazone	Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay	[PMID: 20656494]
CHO	EC₅₀	0.39 μM Compound: Pioglitazone	Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay	[PMID: 21377875]
COS-1	EC₅₀	0.39 μM Compound: 2	Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay	[PMID: 21130649]
COS-7	EC₅₀	0.2 μM Compound: Pioglitazone	Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay	[PMID: 26595749]
COS-7	EC₅₀	0.2 μM Compound: pioglitazone	Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay	[PMID: 23130964]
COS-7	EC₅₀	0.3 μM Compound: Pioglitazone	Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay	[PMID: 21873070]
COS-7	EC₅₀	0.3 μM Compound: pioglitazone	Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay	[PMID: 20307981]
COS-7	EC₅₀	0.32 μM Compound: Pioglitazone	Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay	[PMID: 27569195]
COS-7	EC₅₀	0.5 μM Compound: Pioglitazone	Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay	[PMID: 27560282]
CV-1	EC₅₀	580 nM Compound: Pioglitazone	Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay. Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.	[PMID: 11720854]
HEK293	EC₅₀	0.21 μM Compound: Pioglitazone	Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay	[PMID: 25333853]
HEK293	EC₅₀	0.8 μM Compound: 4	Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay	[PMID: 23102891]
HEK293	EC₅₀	1.1 μM Compound: 1	Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 28465099]
HEK293	IC₅₀	22 μM Compound: 1	Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay	[PMID: 28465099]
HepG2	EC₅₀	0.57 μM Compound: Pioglitazone	Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay	[PMID: 22341573]
HT-1080	IC₅₀	> 100 μM Compound: Pioglitazone	Cytotoxic activity in human HT1080 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Cytotoxic activity in human HT1080 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 28395220]
MDA-MB-231	IC₅₀	> 100 μM Compound: Pioglitazone	Cytotoxic activity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Cytotoxic activity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 28395220]
Mesenchymal stem cells	EC₅₀	0.5 μM Compound: Pio	Induction of adiponectin secretion in human BMMSC cells in presence of IDX induction medium by ELISA assay Induction of adiponectin secretion in human BMMSC cells in presence of IDX induction medium by ELISA assay	[PMID: 37077388]
Mesenchymal stem cells	EC₅₀	0.79 μM Compound: PIO	Induction of adipogenesis in differentiated human BMMSC cells assessed as fold increase in adiponectin level in presence of IDX by ELISA Induction of adipogenesis in differentiated human BMMSC cells assessed as fold increase in adiponectin level in presence of IDX by ELISA	[PMID: 36475432]
Mesenchymal stem cells	EC₅₀	0.9 μM Compound: Pio	Induction of adipogenesis in human differentiated BMMSC cells assessed as increase in adiponectin secretion and measured on 5 day in presence of IDX induction medium by ELISA Induction of adipogenesis in human differentiated BMMSC cells assessed as increase in adiponectin secretion and measured on 5 day in presence of IDX induction medium by ELISA	[PMID: 35859875]
PC-3	IC₅₀	> 100 μM Compound: Pioglitazone	Cytotoxic activity in human PC3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Cytotoxic activity in human PC3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 28395220]
THP-1	IC₅₀	> 50 μM Compound: Pioglitazone	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced IL-1beta secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced IL-1beta secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA	[PMID: 23811092]
THP-1	IC₅₀	18.6 μM Compound: Pioglitazone	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA	[PMID: 24531227]
THP-1	IC₅₀	18.84 μM Compound: Pioglitazone	Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA	[PMID: 23811092]
THP-1	IC₅₀	2.97 mM Compound: Pioglitazone	Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation	[PMID: 30818268]

In Vitro

Pioglitazone (0.5 or 1 μM, 5 days) can completely prevent AGEs (advanced glycation end-products)-induced β-cell necrosis and the increase of caspase-3 thereby avoiding the impaired viability caused by AGEs in pancreatic beta cell line HIT-T15^[2].
? Pioglitazone (1 μM, 1 h) can stimulate insulin secretion induced by low glucose concentration and attenuate the GSSG/GSH ratio in cells cultured with AGEs^[2].

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (70.14 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	2.8055 mL	14.0276 mL	28.0552 mL
5 mM	0.5611 mL	2.8055 mL	5.6110 mL
10 mM	0.2806 mL	1.4028 mL	2.8055 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (5.84 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (28.06 mM); Suspened solution; Need ultrasonic

Purity & Documentation

Purity: 99.89%

Data Sheet (278 KB) SDS (419 KB)

COA (246 KB) HNMR (277 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Kuwabara K, et al. A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose leve [Content Brief]

[2]. Puddu A, et al. Pioglitazone attenuates the detrimental effects of advanced glycation end-products in the pancreatic beta cell line HIT-T15. Regul Pept. 2012 Aug 20;177(1-3):79-84. [Content Brief]

[3]. Kubota N, et al. Pioglitazone ameliorates insulin resistance and diabetes by both adiponectin-dependent and -independent pathways. J Biol Chem. 2006 Mar 31;281(13):8748-55. [Content Brief]

[4]. Elrashidy RA, et al. Pioglitazone attenuates cardiac fibrosis and hypertrophy in a rat model of diabetic nephropathy. J Cardiovasc Pharmacol Ther. 2012 Sep;17(3):324-33. [Content Brief]

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