Pioglitazone (AD-4833)

Catalog No.S2590 Synonyms: U 72107

For research use only.

Pioglitazone (AD-4833, U 72107) is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.

Pioglitazone (AD-4833) Chemical Structure

CAS No. 111025-46-8

Selleck's Pioglitazone (AD-4833) has been cited by 26 publications

Purity & Quality Control

Choose Selective PPAR Inhibitors

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Biological Activity

Description Pioglitazone (AD-4833, U 72107) is a selective peroxisome proliferator-activated receptor-gamma (PPARγ) agonist, used to treat diabetes; A weak activator for full-length hPPARα, but not full-length hPPARδ.
Targets
PPARγ [2]
In vitro

Pioglitazone is metabolised mainly by CYP2C8 and to a lesser extent by CYP3A4 in vitro. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CV-1 M1\FUWZ2dmO2aX;uJIF{e2G7 M3\1T2lvKH[rdILvJJRz[W6|Y4LpdJRqd26jbDDhZ5RqfmG2aX;uJI9nKFCncn;4bZNwdWVicILvcIln\XKjdH;yJIFkfGm4YYTl[EBz\WOncITvdkBo[W2vYTCoVHBCWiliZYjwdoV{e2WmIHnuJGNXNTFiY3XscJMtKEWFNUC9NE43Qc7:TR?= MmDQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQDV5NkmwO{c,QDV5NkmwO|ww[T5?
3T3-L1 MV;GeY5kfGmxbjDhd5NigQ>? MYjF[oZm[3SrdnWgZ49v[2WwdILheIlwdiCob4KgOVAmKGWwaHHuZ4Vu\W62IH;mJIlve3WuaX6tbY5lfWOnZDD0dolodHmlZYLp[IUh[WOldX31cIF1cW:wIHnuJFNVOy2OMTDj[YxteyxiRVO1NF0xNjF4zszN MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86PTl7MkSxK|46PTl7MkSxQE9iRg>?
CV-1 NULpcY5lTnWwY4Tpc44h[XO|YYm= NXvVXmx3SWO2aY\heIlwdiCxZjDw[ZJwgGm|b33lJJBzd2yrZnXyZZRweiCjY4TpeoF1\WRicnXj[ZB1d3JiZ3HtcYEhdWWjc4Xy[YQh[nliaX7keYN1cW:wIH;mJFUxLSCxZjDtZZhqdXWvIHHsb4FtcW6nIIDoc5NxcGG2YYPlJIFkfGm4aYT5MEB1emGwc3\lZ5Rqd25iYYPzZZkhcW5iQ2[tNUBk\WyuczygSWM2OD1yLkW4PFg1|ryP MlPuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwQTh|Nk[yNEc,QTh|Nk[yNFww[T5?
CV-1 M2DZXWZ2dmO2aX;uJIF{e2G7 MlfqUYF5cW2jbDDy[ZBwenSncjDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCncn;4bZNwdWVicILvcIln\XKjdH;yJIFkfGm4YYTl[EBz\WOncITvdkBo[W2vYTDHZYw1KGOqaX3ldolkKGmwIITyZY5{cWWwdHz5JJRz[W6|ZnXjeIVlKEOYLUGgZ4VtdHNiYomg[pVv[3Srb37hcEBie3OjeT6sJGVEPTB;MD61PO69VQ>? Ml7lQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTF5MkC4OVQoRjFzN{KwPFU1RC:jPh?=
HEK293 M4TvcmZ2dmO2aX;uJIF{e2G7 MnLCRYdwdmm|dDDhZ5Rqfmm2eTDheEBRWEGUZ3HtcYEh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCrbnT1Z5Rqd25ib3[gdoVk\XC2b4KgbY51\XKjY4Tpc44hf2m2aDDzeIVzd2mmIILlZ4VxfG:{IHPvZYN1cX[jdH;yMVEh[nliRWnGVEBj[XOnZDDy[ZBwenSncjDn[Y5mKGG|c3H5 NV;R[XdSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[2PFAyPTlpPkG2OlgxOTV7PD;hQi=>
HEK293 M4T3eWZ2dmO2aX;uJIF{e2G7 MX;B[49vcXO2IHHjeIl3cXS7IHH0JHBRSVKpYX3tZUBmgHC{ZYPz[YQhcW5iSFXLNlk{KGOnbHzzJIF{e2W|c3XkJIF{KGmwZIXjeIlwdiCxZjDy[YNmeHSxcjDpcpRmemGldHnvckB4cXSqIILleIlvd2mmIGitdoVk\XC2b4KgZYxxcGFiYomgSXlHWCCkYYPl[EBz\XCxcoTldkBo\W6nIHHzd4F6 M2LFZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NkiwNVU6Lz5zNk[4NFE2QTxxYU6=
CV1 M3;iXWZ2dmO2aX;uJIF{e2G7 MUTUdoFve2GldHn2ZZRqd25ib3[gVHBCWmejbX3hJIlvKEOYMTDj[YxteyxiRVO1NF0xNjV3zszN NXTCVY8xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4NlE4PjlpPkG2PFIyPzZ7PD;hQi=>
Cos7 M2LBVmZ2dmO2aX;uJIF{e2G7 NYno[WRqOTRiaILz MX\UdoFve2GldHn2ZZRqd25ib3[gbJVu[W5iUGDBVodidW2jIFzCSEBmgHC{ZYPz[YQhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR49{PyClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKG[3c3XkJGdCVDRvRFLEJIFnfGW{IEG0JIhzeyCkeTDEeYFtNUeubzDMeYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE4{|ryP NVzG[FBXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCzNFc6QDFpPkKwN|A4QThzPD;hQi=>
3T3L1 M4TkOmZ2dmO2aX;uJIF{e2G7 NIP4VVQyODBidX3vcE9N NXLzemJHUW6lcnXhd4UhcW5iUGDBVodidW2jIH3SUmEhdGW4ZXzzJIlvKG2xdYPlJFNVO0xzIHPlcIx{KGG2IEGwNEB2dW:uL1ygZpkhWlRvUFPS MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODN7Mk[0OUc,OjB|OUK2OFU9N2F-
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COS-1 NI[2T3dHfW6ldHnvckBie3OjeR?= MoLERYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDQVGFT\2GvbXGgcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGW6cILld5Nm\CCrbjDDU3MuOSClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKEejbESgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwM{pOwG0> NGTLOJY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUGzNFY1QSd-MkGxN|A3PDl:L3G+
CHO MUXGeY5kfGmxbjDhd5NigQ>? NGW3XnIzPCCqcoO= NXvI[YN6WGG{dHnhcEBi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHBRSVKpYX3tZUBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHPvMZRz[W6|ZnXjeIVlKHerdHigS4FtPC2{ZYPwc45{cX[nIHz1Z4ln\XKjc3WgdoVxd3K2ZYKgdIxie22rZDDh[pRmeiB{NDDodpMh[nlidILhcpNi[3SrdnH0bY9vKGG|c3H5MEBGSzVyPUCuN|nPxE1? M1TsbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{e3PFc2Lz5{MUO3O|g4PTxxYU6=
COS7 NIHtcmNHfW6ldHnvckBie3OjeR?= NUDLNVhvVW:mdXzheIlwdiCxZjDoeY1idiCSUFHS[4FudWFvTFLEJIV5eHKnc4Pl[EBqdiCjZoLpZ4FvKGe{ZXXuJI1wdmuneTDDU3M4KGOnbHzzJINwNXS{YX7z[oVkfGWmIIfpeIghT2GuNDDhd5Nme3OnZDDhd{Bi[3SrdnH0bY9vKG:oIITyZY5{[WO2aY\heIlwdiCjY4Tpeol1gSCkeTDseYNq\mW{YYPlJIF{e2G7LDDFR|UxRTBwM988US=> NG\DOGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUi3N|A4OCd-MkG4O|MxPzB:L3G+
Sf21 Mk\uSpVv[3Srb36gZZN{[Xl? NE[xUZZKdmirYnn0bY9vKG:oIHj1cYFvKEKVRWCg[ZhxemW|c3XkJIlvKHCuYYPtZUBu\W2kcnHu[UB3\XOrY3zld{Bw\iCVZkKxJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiQWTQMYRmeGWwZHXueEBcO0ifdHH1do9kcG:uYYTlJJVxfGGtZTygTWM2OD1yLkROwG0> NYP0fVFrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkG5OlU3OjNpPkKxPVY2PjJ|PD;hQi=>
Sf21 M3fvemZ2dmO2aX;uJIF{e2G7 NG\5b2lKdmirYnn0bY9vKG:oIGPwdoFofWVvRHH3cIV6KHKjdDDCd4VxKGW6cILld5Nm\CCrbjDwcIF{dWFibXXtZpJidmVidnXzbYNt\XNib3[gV4YzOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGFVWC2mZYDlcoRmdnRiW{PIYZRifXKxY3jvcIF1\SC3cIThb4UtKEmFNUC9Nu69VQ>? M4jtUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[1OlI{Lz5{MUm2OVYzOzxxYU6=
HepG2 MlXhSpVv[3Srb36gZZN{[Xl? MXGyNEBpenN? M4\FXWFod26rc4SgZYN1cX[rdImgZZQhT0GOND30ZYdo\WRiaIXtZY4hWFCDUnfhcY1iKGyrZ3Hu[EBjcW6maX7nJIRwdWGrbjDlfJBz\XO|ZXSgbY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgeJJidnOjY4TpeoF1cW:wIHHmeIVzKDJyIHjyd{BjgSCkZYThMYdidGGldH;zbYRie2VicnXwc5J1\XJiZ3Xu[UBie3OjeTygSWM2OD1yLkW3{txO MkHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ|NEG1O|MoRjJ{M{SxOVc{RC:jPh?=
HEK293 NUP2ZYh{TnWwY4Tpc44h[XO|YYm= NX75XmZLOThiaILz MWHUdoFve2GldHn2ZZRqd25ib3[gbJVu[W5iR1HMOE1nfXOnZDDQVGFT\2GvbXGgcIlo[W6mIHLpcoRqdmdiZH;tZYlvKHS{YX7z[oVkfGWmIHnuJGhGUzJ7MzDj[YxteyCjZoTldkAyQCCqcoOgZpkh\HWjbDDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEWFNUC9NE45|ryP NFLxNJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{GwNlg6OSd-MkOxNFI5QTF:L3G+
COS7 MnnySpVv[3Srb36gZZN{[Xl? MlfRWJJidnOjY4TpeoF1cW:wIH;mJGdCVDRvZoXz[YQhcHWvYX6gVHBCWmejbX3hJIxq\2GwZDDibY5lcW6pIHTvcYFqdiC2cnHud4Zm[3SnZDDpckBi\nKrY3HuJIdz\WWwIH3vcotmgSCFT2O3JINmdGy|IHL5JIx2[2moZYLhd4UhemWyb4L0[ZIh\2WwZTDhd5NigSxiRVO1NF0xNjMQvF2= NYDsU2t[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxN|A6PjRpPkKzNVMxQTZ2PD;hQi=>
THP1 NYnkXlk{SW62aXnu[oxidW2jdH;yfUBie3OjeR?= NXXuZ21lOSCqch?= MVzBcpRqcW6obHHtcYF1d3K7IHHjeIl3cXS7IHnuJIh2dWGwIGTIVFEh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDQUWEucW6mdXPl[EBOS1BvMTDz[YNz\XSrb36gdJJmcW6ldXLheIVlKG[xcjCxJIhzKHC{aX;yJHBOSS2laHHscIVv\2VibXXhd5Vz\WRiYX\0[ZIhPDhiaILzJIJ6KEWOSWPBMEBKSzVyPUG4Mlg1|ryP MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzhzMUC5Nkc,OjN6MUGwPVI9N2F-
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Assay
Methods Test Index PMID
Western blot p-VEGFR2 / VEGFR ; Phopsho-RB / RB 29972411 25264247
In vivo Pioglitazone significantly attenuates left ventricular (LV) cavity dilatation and dysfunction by echocardiography as well as LV end-diastolic pressure in mice with extensive anterior myocardial infarction. Pioglitazone partially normalizes LV dP/dt(max) and dP/dt(min), indices of LV contractile function, which are significantly reduced in MI mice. [2] Pioglitazone results in a reduced activation of microglia, reduced induction of iNOS-positive cells and less glial fibrillary acidic protein positive cells in both striatum and substantia nigra pars compacta of MPTP mouse model of Parkinson's disease. Pioglitazone almost completely blocks staining of TH-positive neurons for nitrotyrosine, a marker of NO-mediated cell damage. [3] Pioglitazone (approximately 20 mg/kg/day) attenuates the MPTP-induced glial activation and prevents the dopaminergic cell loss in the substantia nigra pars compacta (SNpc) in MPTP mouse model of Parkinson's disease. [4] Pioglitazone results in a reduction in the number of activated microglia and reactive astrocytes in the hippocampus and cortex of 10-month-old APPV717I transgenic mice. Pioglitazone treatment reduces the expression of the proinflammatory enzymes cyclooxygenase 2 (COX2) and inducible nitric oxide synthase (iNOS). Pioglitazone decreases beta-secretase-1 (BACE1) mRNA and protein levels, and also a 27% reduction in the levels of soluble Abeta1-42 peptide. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 356.44
Formula

C19H20N2O3S

CAS No. 111025-46-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=CN=C(C=C1)CCOC2=CC=C(C=C2)CC3C(=O)NC(=O)S3

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Working concentration: mg/ml;

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04501406 Recruiting Drug: Pioglitazone|Other: Placebo Type 2 Diabetes Mellitus (T2DM)|Nonalcoholic Steatohepatitis University of Florida|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK) December 15 2020 Phase 2
NCT04535700 Recruiting Drug: Pioglitazone 30 mg|Other: standard of care Type 2 Diabetes Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal September 18 2020 Phase 4
NCT00904046 Recruiting Drug: Pioglitazone|Drug: Placebo Uric Acid Kidney Stone Disease University of Texas Southwestern Medical Center|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Takeda Pharmaceuticals North America Inc. September 5 2019 Not Applicable
NCT04671056 Completed Drug: MGL-3196|Drug: Pioglitazone 15mg Healthy Madrigal Pharmaceuticals Inc. November 9 2018 Phase 1
NCT03501277 Completed Drug: Alogliptin|Drug: Pioglitazone|Drug: SYR-322-4833 BL Healthy Volunteers Takeda May 26 2018 Phase 1
NCT03471117 Recruiting Drug: Pioglitazone|Other: Placebo Chronic Kidney Diseases The University of Texas at Arlington|University of Texas Southwestern Medical Center at Dallas April 1 2018 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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