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 MWTGeY5kfGmxbjDhd5NigQ>? NUfrXI5QUW5idnn0do8hfHKjboPjdolxfGmxbnHsJIFkfGm4YYTpc44hd2ZiUHXyc5hqe2:vZTDwdo9tcW[ncnH0c5Ih[WO2aY\heIVlKHKnY3XweI9zKGejbX3hJEhRWEGUKTDlfJBz\XO|ZXSgbY4hS1ZvMTDj[YxteyxiRVO1NF0xNjZ7zszN NHXPVpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi96NUe2PVA4Lz56NUe2PVA4RC:jPh?=
3T3-L1 NILTe|FHfW6ldHnvckBie3OjeR?= MlewSYZn\WO2aY\lJINwdmOnboTyZZRqd25iZn;yJFUxLSCnbnjhcoNmdWWwdDDv[kBqdnO3bHnuMYlv\HWlZXSgeJJq\2y7Y3XybYRmKGGlY4XteYxifGmxbjDpckA{XDNvTEGgZ4VtdHNuIFXDOVA:OC5zNt88US=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek86PTl7MkSxK|46PTl7MkSxQE9iRg>?
CV-1 MkL3SpVv[3Srb36gZZN{[Xl? M1O3[mFkfGm4YYTpc44hd2ZicHXyc5hqe2:vZTDwdo9tcW[ncnH0c5Ih[WO2aY\heIVlKHKnY3XweI9zKGejbX3hJI1m[XO3cnXkJIJ6KGmwZIXjeIlwdiCxZjC1NEUhd2ZibXH4bY12dSCjbHvhcIlv\SCyaH;zdIhifGG|ZTDhZ5Rqfmm2eTygeJJidnOoZXP0bY9vKGG|c3H5JIlvKEOYLUGgZ4VtdHNuIFXDOVA:OC53OEi4OO69VQ>? M1\Rc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493Nzl6M{[2NlAoRjl6M{[2NlA9N2F-
CV-1 MWPGeY5kfGmxbjDhd5NigQ>? MXLNZZhqdWGuIILldI9zfGW{IHHjeIl3cXS7IHHnZYlve3RiaIXtZY4hWGW{b4jpd49u\SCycn;sbYZmemG2b4KgZYN1cX[jdHXkJJJm[2WydH;yJIdidW2jIFfhcFQh[2irbXXybYMhcW5idILhcpNq\W62bImgeJJidnOoZXP0[YQhS1ZvMTDj[YxteyCkeTDmeY5kfGmxbnHsJIF{e2G7LjygSWM2OD1yLkW4{txO NGfWeog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zMUeyNFg2PCd-MUG3NlA5PTR:L3G+
HEK293 MnrWSpVv[3Srb36gZZN{[Xl? M2fZWGFod26rc4SgZYN1cX[rdImgZZQhWFCDUnfhcY1iKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7keYN1cW:wIH;mJJJm[2WydH;yJIlvfGW{YXP0bY9vKHerdHigd5Rmem:rZDDy[YNmeHSxcjDjc4FkfGm4YYTvdk0yKGK7IFXZSnAh[mG|ZXSgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> M4HPR|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4NkiwNVU6Lz5zNk[4NFE2QTxxYU6=
HEK293 MX\GeY5kfGmxbjDhd5NigQ>? M{DFbGFod26rc4SgZYN1cX[rdImgZZQhWFCDUnfhcY1iKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiaX7keYN1cW:wIH;mJJJm[2WydH;yJIlvfGW{YXP0bY9vKHerdHigdoV1cW6xaXSgXE1z\WOncITvdkBidHCqYTDifUBGYU[SIHLhd4VlKHKncH;yeIVzKGenbnWgZZN{[Xl? MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjZ6MEG1PUc,OTZ4OECxOVk9N2F-
CV1 NEW5coVHfW6ldHnvckBie3OjeR?= MWrUdoFve2GldHn2ZZRqd25ib3[gVHBCWmejbX3hJIlvKEOYMTDj[YxteyxiRVO1NF0xNjV3zszN NVvPVZlGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4NlE4PjlpPkG2PFIyPzZ7PD;hQi=>
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HEK293T MoTTSpVv[3Srb36gZZN{[Xl? NXruVGNKOSC3TR?= MX2yOEBpenN? NXn3SFVSWGG{dHnhcEBi\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHBRSVKpYX3tZU1NSkRiZYjwdoV{e2WmIHnuJGhGUzJ7M2SgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5lfWO2aX;uJI9nKHKnY3XweI9zKHS{YX7zZYN1cX[jdHnvckBifCBzIIXNJIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZk> Mle1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFyM{CyOlMoRjJzMEOwNlY{RC:jPh?=
COS-1 M3jRSWZ2dmO2aX;uJIF{e2G7 MoX5RYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDQVGFT\2GvbXGgcIlo[W6mIHLpcoRqdmdiZH;tZYlvKGW6cILld5Nm\CCrbjDDU3MuOSClZXzsd{Bkdy22cnHud4Zm[3SnZDD3bZRpKEejbESgZpkhdHWlaX\ldoF{\SC{ZYDvdpRmeiCpZX7lJIF{e2G7LDDFR|UxRTBwM{pOwG0> Mn7hQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjFzM{C2OFkoRjJzMUOwOlQ6RC:jPh?=
CHO MWLGeY5kfGmxbjDhd5NigQ>? MUWyOEBpenN? MWnQZZJ1cWGuIHHnc45qe3RiYXP0bZZqfHliYYSgbJVu[W5iUGDBVodidW2jIHX4dJJme3OnZDDpckBEUE9iY3XscJMh[29vdILhcpNn\WO2ZXSge4l1cCCJYXy0MZJme3CxboPpeoUhdHWlaX\ldoF{\SC{ZYDvdpRmeiCybHHzcYllKGGodHXyJFI1KGi{czDifUB1emGwc3HjeIl3[XSrb36gZZN{[XluIFXDOVA:OC5|Od88US=> MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5N{i3OUc,OjF|N{e4O|U9N2F-
COS7 MXrGeY5kfGmxbjDhd5NigQ>? NF;m[ZBOd2S3bHH0bY9vKG:oIHj1cYFvKFCSQWLnZY1u[S2OQlSg[ZhxemW|c3XkJIlvKGGocnnjZY4h\3KnZX6gcY9vc2W7IFPPV|ch[2WubIOgZ48ufHKjboPm[YN1\WRid3n0bEBI[Wx2IHHzd4V{e2WmIHHzJIFkfGm4YYTpc44hd2ZidILhcpNi[3SrdnH0bY9vKGGldHn2bZR6KGK7IHz1Z4ln\XKjc3WgZZN{[XluIFXDOVA:OC5|zszN M2TKNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOEezNFcxLz5{MUi3N|A4ODxxYU6=
Sf21 NXLlZopQTnWwY4Tpc44h[XO|YYm= M2X6bWlvcGmkaYTpc44hd2ZiaIXtZY4hSlOHUDDlfJBz\XO|ZXSgbY4heGyjc33hJI1mdWK{YX7lJJZme2mlbHXzJI9nKFOoMkGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCDVGCt[IVx\W6mZX70JHs{UF22YYXyc4Npd2yjdHWgeZB1[WunLDDJR|UxRTBwM988US=> M4Pz[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[1OlI{Lz5{MUm2OVYzOzxxYU6=
Sf21 MmjlSpVv[3Srb36gZZN{[Xl? NIHQUHdKdmirYnn0bY9vKG:oIGPwdoFofWVvRHH3cIV6KHKjdDDCd4VxKGW6cILld5Nm\CCrbjDwcIF{dWFibXXtZpJidmVidnXzbYNt\XNib3[gV4YzOSClZXzsd{Bie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGFVWC2mZYDlcoRmdnRiW{PIYZRifXKxY3jvcIF1\SC3cIThb4UtKEmFNUC9Nu69VQ>? M{jQdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOU[1OlI{Lz5{MUm2OVYzOzxxYU6=
HepG2 MnLJSpVv[3Srb36gZZN{[Xl? M3XUPVIxKGi{cx?= NWO5bII4SWexbnnzeEBi[3Srdnn0fUBifCCJQVy0MZRi\2enZDDoeY1idiCSUFHS[4FudWFibHnnZY5lKGKrbnTpcoch\G:vYXnuJIV5eHKnc4Pl[EBqdiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{B1emGwc3HjeIl3[XSrb36gZYZ1\XJiMkCgbJJ{KGK7IHLleIEu\2GuYXP0c5Nq\GG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBGSzVyPUCuOVfPxE1? M4DHdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{M{SxOVc{Lz5{MkO0NVU4OzxxYU6=
HEK293 MlvGSpVv[3Srb36gZZN{[Xl? NX\JWllsOThiaILz NG\3Vo9VemGwc3HjeIl3[XSrb36gc4YhcHWvYX6gS2FNPC2odYPl[EBRWEGUZ3HtcYEhdGmpYX7kJIJqdmSrbneg[I9u[WmwIITyZY5{\mWldHXkJIlvKEiHS{K5N{Bk\WyuczDh[pRmeiBzODDodpMh[nliZIXhcEBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[XluIFXDOVA:OC56zszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzFyMki5NUc,OjNzMEK4PVE9N2F-
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THP1 Ml\hRY51cWmwZnzhcY1ifG:{eTDhd5NigQ>? NH\MeZAyKGi{ NVvWUGtFSW62aXnu[oxidW2jdH;yfUBi[3Srdnn0fUBqdiCqdX3hckBVUFBzIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhWE2DLXnu[JVk\WRiTVPQMVEhe2WlcnX0bY9vKHC{ZXnuZ5Vj[XSnZDDmc5IhOSCqcjDwdolweiCSTVGtZ4hidGynbnflJI1m[XO3cnXkJIFnfGW{IES4JIhzeyCkeTDFUGlUSSxiSVO1NF0yQC56NN88US=> M1zzb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEGxNFkzLz5{M{ixNVA6OjxxYU6=
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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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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05411965 Completed Drug: BR3003(T)|Drug: BR3003B(R1)|Drug: BR3003C(R2) Diabetes Mellitus Type 2 Boryung Pharmaceutical Co. Ltd April 28 2022 Phase 1
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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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