Rosiglitazone
Based on 189 publication(s) in Google Scholar
Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.94%
- CAS No.: 122320-73-4
- 화학식: C18H19N3O3S
- 분자량:357.43
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Rosiglitazone
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- Nucleic Acids Res. 2025 Jul 19;53(14):gkaf669. [Abstract]
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- Ocul Surf. 2024 Oct:34:444-458. [Abstract]
- Ecotoxicol Environ Saf. 2022 Jun 15;238:113611. [Abstract]
- Cell Mol Life Sci. 2025 Nov 19;82(1):412. [Abstract]
- Life Sci. 2021 Mar 15:269:119013. [Abstract]
- Compr Physiol. 2026 Jun;16(3):e70175. [Abstract]
- Biomed J. 2025 Oct 9:100916. [Abstract]
- Mol Metab. 2024 Oct 29:102053. [Abstract]
- Food Funct. 2019 Dec 11;10(12):7983-7994. [Abstract]
- Inflamm Res. 2024 Oct;73(10):1765-1780. [Abstract]
- Cells. 2026 Apr 13;15(8):684. [Abstract]
- Cells. 2026 Feb 11;15(4):329. [Abstract]
- Cells. 2021 Dec 28;11(1):86. [Abstract]
- Nutrients. 2025 Feb 25;17(5):794. [Abstract]
- Commun Biol. 2024 Apr 9;7(1):429. [Abstract]
- Eur J Pharmacol. 2025 Jun 5:996:177445. [Abstract]
- Eur J Pharmacol. 2023 Dec 5:960:176113. [Abstract]
- Pharmaceuticals (Basel). 2022 Aug 26;15(9):1055. [Abstract]
- Eur J Pharmacol. 2022 Sep 15:931:175175. [Abstract]
- J Zhejiang Univ Sci B. 2020;21(12):990-998. [Abstract]
- Eur J Pharmacol. 2020 Sep 5;882:173300. [Abstract]
- Eur J Pharmacol. 2019 Jan 15:843:134-144. [Abstract]
- Int J Mol Sci. 2026 May 10;27(10):4255. [Abstract]
- Int Immunopharmacol. 2026 Jan 1;168(Pt 1):115739. [Abstract]
- Int J Mol Sci. 2025 Oct 18;26(20):10132. [Abstract]
- Int J Mol Sci. 2025 Apr 10;26(8):3553. [Abstract]
- Int Immunopharmacol. 2021 Jan;90:107150. [Abstract]
- Am J Physiol Cell Physiol. 2026 Jan 1;330(1):C142-C154. [Abstract]
- Front Pharmacol. 2022 Jun 27;13:919202. [Abstract]
- Front Cell Dev Biol. 2020 Jul 29;8:703. [Abstract]
- Bioorg Chem. 2026 Jul 5:175:109764. [Abstract]
- Molecules. 2024 Oct 15;29(20):4881. [Abstract]
- Bioorg Chem. 2022 Dec:129:106191. [Abstract]
- J Physiol Biochem. 2022 May;78(2):377-388. [Abstract]
- Food Sci Nutr. 2026 Jan 7;14(1):e71429. [Abstract]
- Food Sci Nutr. 2025 Sep 22;13(9):e71009. [Abstract]
- J Lipid Res. 2026 Feb;67(2):100981. [Abstract]
- Sci Rep. 2024 Apr 30;14(1):9960. [Abstract]
- Exp Neurol. 2025 Oct 11:395:115486. [Abstract]
- Mol Cell Biochem. 2026 Mar 13. [Abstract]
- J Drug Target. 2025 Jul 17:1-10. [Abstract]
- Cell Signal. 2022 May:93:110299. [Abstract]
- J Cell Mol Med. 2019 Oct;23(10):7029-7042. [Abstract]
- Poult Sci. 2026 Jan 18;105(4):106481. [Abstract]
- iScience. 2026 Jan 7;29(2):114638. [Abstract]
- iScience. 2023 Feb 28;26(4):106289. [Abstract]
- iScience. 2022 Oct 10;25(11):105319. [Abstract]
- Biomedicines. 2021 Jun 15;9(6):677. [Abstract]
- Aquaculture. 2026 Jan 4;615:743618.
- Aquaculture. 2024 Jan 15, 578, 740081.
- Front Mol Biosci. 2022 Feb 4;8:766887. [Abstract]
- Front Mol Neurosci. 2017 Sep 14;10:293. [Abstract]
- Front Physiol. 2019 Mar 1:10:165. [Abstract]
- Am J Physiol Endocrinol Metab. 2024 May 1;326(5):E696-E708. [Abstract]
- Drug Dev Res. 2023 Aug;84(5):922-936. [Abstract]
- Prog Neuropsychopharmacol Biol Psychiatry. 2023 Jul 13:125:110758. [Abstract]
- Clin Immunol. 2026 Apr:284:110677. [Abstract]
- J Biol Chem. 2024 Sep 12:107765. [Abstract]
- J Cell Physiol. 2019 Nov;234(11):20694-20703. [Abstract]
- Neuromolecular Med. 2025 Jan 27;27(1):12. [Abstract]
- Carcinogenesis. 2023 May 27;44(3):242-251. [Abstract]
- Ren Fail. 2022 Dec;44(1):2056-2065. [Abstract]
- Biochim Biophys Acta Mol Cell Biol Lipids. 2020 Aug;1865(8):158711. [Abstract]
- J Biochem Mol Toxicol. 2026 Feb;40(2):e70701. [Abstract]
- J Biochem Mol Toxicol. 2025 Oct;39(10):e70484. [Abstract]
- Exp Cell Res. 2026 Jun 9;461(1):115102. [Abstract]
- Exp Cell Res. 2026 May 1;458(1):114947. [Abstract]
- Bioorg Med Chem. 2022 Feb 15:56:116615. [Abstract]
- PPAR Res. 2023 Nov 8:2023:6422804. [Abstract]
- PPAR Res. 2022 Sep 28:2022:7888937. [Abstract]
- Adipocyte. 2021 Dec;10(1):646-657. [Abstract]
- PPAR Res. 2019 Jul 1:2019:2715176. [Abstract]
- BMC Gastroenterol. 2025 Jan 20;25(1):22. [Abstract]
- J Therm Biol. 2024 Jul 2:123:103906. [Abstract]
- Front Vet Sci. 2023 Nov 17:10:1277586. [Abstract]
- Am J Cancer Res. 2020 Apr 1;10(4):1182-1193. [Abstract]
- Fish Physiol Biochem. 2025 Feb 15;51(2):51. [Abstract]
- Orthod Craniofac Res. 2025 Jun 28. [Abstract]
- J Cardiovasc Transl Res. 2024 Dec;17(6):1415-1426. [Abstract]
- Biochem Biophys Res Commun. 2026 Jul 23:823:153971. [Abstract]
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- Endocr J. 2022 Apr 28;69(4):385-397. [Abstract]
- Biochem Biophys Res Commun. 2020 Mar 26;524(1):70-76. [Abstract]
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- Reprod Domest Anim. 2023 Nov;58(11):1559-1568. [Abstract]
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RT-PCR
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WB
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RT-PCR
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WB
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Cell Proliferation/Viability Assay
Biological Activity
|
PPARγ 40 nM (Kd) |
PPARγ 60 nM (EC50) |
TRPC5 30 μM (EC50) |
TRPM3 |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 3T3-L1 | EC50 |
1.72 μM
Compound: 1; Rosi
|
Induction of insulin-stimulated 2-NBDG uptake in TNF-alpha-induced insulin resistant mouse 3T3L1 cells preincubated for 48 hrs followed by 2-NBDG addition measured after 30 mins in presence of insulin by fluorescence assay
Induction of insulin-stimulated 2-NBDG uptake in TNF-alpha-induced insulin resistant mouse 3T3L1 cells preincubated for 48 hrs followed by 2-NBDG addition measured after 30 mins in presence of insulin by fluorescence assay
|
[PMID: 30481687] |
| 3T3-L1 | EC50 |
0.12 μM
Compound: Rosiglitazone
|
Antidiabetic activity in mouse 3T3L1 preadipocytes assessed as increase in triglycerides level after 6 days
Antidiabetic activity in mouse 3T3L1 preadipocytes assessed as increase in triglycerides level after 6 days
|
[PMID: 32130008] |
| BHK-21 | EC50 |
0.45 μM
Compound: RSG
|
Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay
Agonist activity at human PPARgamma expressed in BHK21 cells assessed as SEAP activity by luciferase reporter transactivation assay
|
[PMID: 19349176] |
| CHO | IC50 |
29.5 μM
Compound: 1; Rosi
|
Inhibition of human ERG expressed in CHO cells by patch clamp assay
Inhibition of human ERG expressed in CHO cells by patch clamp assay
|
[PMID: 30481687] |
| CHO-K1 | EC50 |
0.1 μM
Compound: Rosiglitazone
|
Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay
Partial agonist activity at human PPARgamma-LBD expressed in CHO-K1 cells co-transfected with GAL4 assessed as luciferase activity by transactivation assay
|
[PMID: 20527969] |
| COS-1 | EC50 |
21 nM
Compound: Rosiglitazone
|
Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor
Agonistic activity was determined in COS1 cells transfected with GAL 4-PPAR gamma receptor
|
[PMID: 12617924] |
| COS-1 | EC50 |
>3 μM
Compound: Rosiglitazone
|
In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells
In vitro agonist activity tested for transactivation in human PPAR alpha-Gal4 chimeric COS-1 cells
|
[PMID: 12729668] |
| COS-1 | EC50 |
>3 μM
Compound: Rosiglitazone
|
In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells
In vitro agonist activity tested for transactivation in human PPAR delta-GAL4 chimeric COS-1 cells
|
[PMID: 12729668] |
| COS-1 | EC50 |
0.02 μM
Compound: Rosiglitazone
|
In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells
In vitro agonist activity tested for transactivation in human PPAR gamma-Gal4 chimeric COS-1 cells
|
[PMID: 12729668] |
| COS-1 | EC50 |
>3 μM
Compound: Rosiglitazone
|
In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell
In vitro transactivation of human Peroxisome proliferator activated receptor alpha measured in PPAR-GAL4 chimeric COS-1 cell
|
[PMID: 12873517] |
| COS-1 | EC50 |
>3 μM
Compound: Rosiglitazone
|
In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells
In vitro transactivation of human Peroxisome proliferator activated receptor delta measured in PPAR-GAL4 chimeric COS-1 cells
|
[PMID: 12873517] |
| COS-1 | EC50 |
0.02 μM
Compound: Rosiglitazone
|
In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells
In vitro transactivation of human peroxisome proliferator activated receptor gamma measured in PPAR-GAL4 chimeric COS-1 cells
|
[PMID: 12873517] |
| COS-1 | EC50 |
0.023 μM
Compound: Rosiglitazone
|
In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay
In vitro maximal activation of human Peroxisome proliferator activated receptor gamma in COS-1 cell transactivation assay
|
[PMID: 15603954] |
| COS-1 | EC50 |
20 nM
Compound: rosiglitazone
|
Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay
Agonist activity at human recombinant PPARgamma expressed in COS1 cells co-expressing GAL4 assessed as transcriptional activity after 48 hrs by luciferase reporter gene assay
|
[PMID: 19507861] |
| COS-1 | EC50 |
>3000 nM
Compound: Rosiglitazone
|
Agonist activity at mouse PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
Agonist activity at mouse PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
|
[PMID: 19530681] |
| COS-1 | EC50 |
20 nM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
Agonist activity at human PPARgamma receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
|
[PMID: 19530681] |
| COS-1 | EC50 |
>3000 nM
Compound: Rosiglitazone
|
Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
Agonist activity at human PPARalpha receptor expressed in african green monkey COS1 cells co-transfected with fused yeast Gal4-DBD by transactivation assay
|
[PMID: 19530681] |
| COS-1 | EC50 |
>1000 nM
Compound: BRL
|
Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
|
[PMID: 22051054] |
| COS-1 | EC50 |
48 nM
Compound: BRL
|
Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
|
[PMID: 22051054] |
| COS-1 | EC50 |
>1000 nM
Compound: BRL
|
Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
|
[PMID: 22051054] |
| COS-1 | EC50 |
0.12 μM
Compound: Rosiglitazone
|
Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay
Transactivation of human full length PPARgamma expressed in COS1 cells co-transfected with RXRalpha after 24 hrs by luciferase reporter gene assay
|
[PMID: 22197396] |
| COS-7 | EC50 |
>10 μM
Compound: 4
|
Agonist activity at human recombinant PPARalpha LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay
Agonist activity at human recombinant PPARalpha LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay
|
[PMID: 20138762] |
| COS-7 | EC50 |
0.03 μM
Compound: 4
|
Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay
Agonist activity at human recombinant PPARgamma1 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay
|
[PMID: 20138762] |
| COS-7 | EC50 |
0.1 μM
Compound: 4
|
Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay
Agonist activity at human recombinant PPARgamma2 LBD expressed in african green monkey COS7 cells coexpressing GAL4 by luciferase reporter gene transactivation assay
|
[PMID: 20138762] |
| COS-7 | EC50 |
0.043 μM
Compound: Rosiglitazone
|
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] |
| CV-1 | EC50 |
43 nM
Compound: Rosiglitazone
|
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] |
| CV-1 | EC50 |
325 nM
Compound: BRL-49653, rosiglitazone
|
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
In vitro evaluation against RXR-alpha/PPAR-gamma in CV-1 cells by cotransfection assay was determined
|
[PMID: 12954061] |
| CV-1 | EC50 |
0.076 μM
Compound: rosiglitazone
|
Transactivation of PPARgamma in CV1 cells
Transactivation of PPARgamma in CV1 cells
|
[PMID: 16821769] |
| CV-1 | EC50 |
308 nM
Compound: Rosiglitazone
|
Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay
Transactivation of human PPARgamma in CV1 cells by luciferase reporter gene assay
|
[PMID: 16970391] |
| CV-1 | EC50 |
308 nM
Compound: 3, Rosigilitazone
|
Activity at human PPARgamma in CV1 cells
Activity at human PPARgamma in CV1 cells
|
[PMID: 17005394] |
| CV-1 | EC50 |
308 nM
Compound: rosiglitazone
|
Agonist activity at PPARgamma in CV1 cells by transactivation assay
Agonist activity at PPARgamma in CV1 cells by transactivation assay
|
[PMID: 17129725] |
| CV-1 | EC50 |
0.03 μM
Compound: rosiglitazone
|
Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs
Agonist activity at human PPARgamma in CV1 cells by GAL4 transactivation assay after 24 hrs
|
[PMID: 17507225] |
| CV-1 | EC50 |
3.46 μM
Compound: rosiglitazone
|
Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs
Agonist activity at human PPARalpha in CV1 cells by GAL4 transactivation assay after 24 hrs
|
[PMID: 17507225] |
| CV-1 | EC50 |
308 nM
Compound: rosiglitazone
|
Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay
Agonist activity at human PPARgamma expressed in CV1 cells by receptor transactivation assay
|
[PMID: 18029178] |
| CV-1 | EC50 |
0.033 μM
Compound: rosiglitazone
|
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 |
3.46 μM
Compound: rosiglitazone
|
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] |
| CV-1 | EC50 |
>10 μM
Compound: Rosiglitazone
|
Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
|
[PMID: 21112784] |
| CV-1 | EC50 |
>10 μM
Compound: Rosiglitazone
|
Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
|
[PMID: 21112784] |
| CV-1 | EC50 |
0.1 μM
Compound: Rosiglitazone
|
Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
|
[PMID: 21112784] |
| CV-1 | EC50 |
>10 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
|
[PMID: 21515063] |
| CV-1 | EC50 |
>10 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
|
[PMID: 21515063] |
| CV-1 | EC50 |
0.1 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
|
[PMID: 21515063] |
| CV-1 | EC50 |
0.06 μM
Compound: 6
|
In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells
|
[PMID: 8576907] |
| CV-1 | EC50 |
50 nM
Compound: 1
|
Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells
Tested for transactivation of human PPAR gamma-Gal4 chimera in CV-1 cells
|
10.1016/S0960-894X(97)10017-8 |
| DU-145 | IC50 |
16 μM
Compound: Rosiglitazone
|
Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human DU145 cells assessed as growth inhibition after 48 hrs by MTT assay
|
[PMID: 24996143] |
| HEK293 | EC50 |
0.035 μM
Compound: rosiglitazone
|
Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARgamma receptor expressed in HEK293 cells by GAL4 transactivation assay
|
[PMID: 17292606] |
| HEK293 | EC50 |
>10 μM
Compound: rosiglitazone
|
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
|
[PMID: 17343371] |
| HEK293 | EC50 |
0.31 μM
Compound: rosiglitazone
|
Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
|
[PMID: 17343371] |
| HEK293 | EC50 |
0.12 μM
Compound: Rosiglitazone
|
Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction
Agonist activity at PPARgamma expressed in HEK293 cells assessed as aP2 gene induction
|
[PMID: 18029176] |
| HEK293 | EC50 |
0.19 μM
Compound: Rosiglitazone
|
Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARgamma expressed in HEK293 cells by GAL4 transactivation assay
|
[PMID: 18029176] |
| HEK293 | EC50 |
>5 μM
Compound: rosiglitazone
|
Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARalpha in HEK293 cells by GAL4 transactivation assay
|
[PMID: 18291645] |
| HEK293 | EC50 |
0.045 μM
Compound: rosiglitazone
|
Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay
Agonist activity at PPARgamma in HEK293 cells by GAL4 transactivation assay
|
[PMID: 18291645] |
| HEK293 | EC50 |
0.035 μM
Compound: Rosiglitazone
|
Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay
Agonist activity at human GAL4-tagged PPARgamma chimeric receptor expressed in HEK cells by transactivation assay
|
[PMID: 20299214] |
| HEK293 | EC50 |
10.58 μM
Compound: Rosiglitazone
|
Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay
Agonist activity at human GAL4-tagged PPARalpha chimeric receptor expressed in HEK cells by transactivation assay
|
[PMID: 20299214] |
| HEK293 | EC50 |
43 nM
Compound: Rosiglitazone
|
Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay
Transactivation of Gal4-fused human PPARgamma expressed in HEK293 cells after 16 to 20 hrs by luciferase reporter gene assay
|
[PMID: 21128600] |
| HEK293 | EC50 |
43.71 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay
|
[PMID: 23265844] |
| HEK293 | EC50 |
0.004 μM
Compound: Rosiglitazone
|
Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay
Agonist at human PPARgamma LBD expressed in human HEK293 cells cotransfected with GAL4-Luc assessed as transcriptional activation by luciferase reporter gene assay
|
[PMID: 23286787] |
| HEK293 | EC50 |
0.1 μM
Compound: 1, Avandia
|
Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
Transactivation of GAL4 DBD-fused human PPARgamma-LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
|
[PMID: 23294830] |
| HEK293 | EC50 |
0.03 μM
Compound: rosiglitazone
|
Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay
Agonist activity at mouse PPARgamma expressed in HEK293 cells co-expressing with Gal4 reporter vector after 24 hrs by dual-luciferase reporter assay
|
[PMID: 24955889] |
| HEK293 | EC50 |
10 nM
Compound: RGZ
|
Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay
Agonist activity at human PPARgamma expressed in HEK293 cells by luciferase reporter gene assay
|
[PMID: 25305688] |
| HEK293 | EC50 |
0.26 μM
Compound: Rosiglitazone
|
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
|
[PMID: 27591006] |
| HEK293 | EC50 |
0.26 μM
Compound: Rosiglitazone
|
Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
Agonist activity at N-terminal Gal4 fused human PPARgamma LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
|
[PMID: 27622746] |
| HEK293 | EC50 |
1.1 μM
Compound: 2
|
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: 2
|
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] |
| HEK293 | EC50 |
0.3 μM
Compound: Rosiglitazone
|
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 |
0.039 μM
Compound: Rosiglitazone
|
Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay
Transactivation of human PPARgamma expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay
|
10.1039/C5MD00151J |
| HeLa | EC50 |
>10000 nM
Compound: 1
|
Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
|
[PMID: 19275963] |
| HeLa | EC50 |
15 nM
Compound: 1
|
Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
|
[PMID: 19275963] |
| HeLa | EC50 |
>10000 nM
Compound: 1
|
Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
|
[PMID: 19275963] |
| Hepatocyte | IC50 |
165 μM
Compound: Rosiglitazone
|
Cytotoxicity against rat primary hepatocytes after 16 hrs
Cytotoxicity against rat primary hepatocytes after 16 hrs
|
10.1039/C3MD00377A |
| Hepatocyte | IC50 |
225 μM
Compound: Rosiglitazone
|
Cytotoxicity against rat primary hepatocytes after 6 hrs
Cytotoxicity against rat primary hepatocytes after 6 hrs
|
10.1039/C3MD00377A |
| HepG2 | EC50 |
0.039 μM
Compound: rosiglitazone
|
Effective concentration against human PPARgamma expressed in HepG2 cells
Effective concentration against human PPARgamma expressed in HepG2 cells
|
[PMID: 16107150] |
| HepG2 | EC50 |
>10 μM
Compound: rosiglitazone
|
Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPAR alpha in a HepG2 cells by PPAR-GAL4 transactivation assay
|
[PMID: 16973358] |
| HepG2 | EC50 |
0.158 μM
Compound: rosiglitazone
|
Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assay
|
[PMID: 16973358] |
| HepG2 | EC50 |
>10 μM
Compound: Rosiglitazone
|
Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPAR alpha in HepG2 cells by PPAR-GAL4 transactivation assay
|
[PMID: 16979341] |
| HepG2 | EC50 |
0.158 μM
Compound: Rosiglitazone
|
Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPAR gamma in HepG2 cells by PPAR-GAL4 transactivation assay
|
[PMID: 16979341] |
| HepG2 | EC50 |
82 nM
Compound: 1,rosiglitazone
|
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 |
>12 μM
Compound: 1, Rosi
|
Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay
Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay
|
[PMID: 18394907] |
| HepG2 | EC50 |
0.223 μM
Compound: 1, Rosi
|
Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay
Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay
|
[PMID: 18394907] |
| HepG2 | EC50 |
0.05 μM
Compound: Rosiglitazone
|
Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
Agonist activity at PPARgamma expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control
|
[PMID: 18625559] |
| HepG2 | EC50 |
0.039 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay
|
[PMID: 18835719] |
| HepG2 | EC50 |
0.04 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
Agonist activity at human PPARgamma ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay
|
[PMID: 19053776] |
| HepG2 | EC50 |
0.039 μM
Compound: rosiglitazone
|
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay
|
[PMID: 19775169] |
| HepG2 | EC50 |
>12 μM
Compound: 3
|
Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay
Agonist activity at human PPARalpha expressed in HepG2 cells by GAL4 transactivation assay
|
[PMID: 19783444] |
| HepG2 | EC50 |
0.223 μM
Compound: 3
|
Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay
Agonist activity at human PPARgamma expressed in HepG2 cells by GAL4 transactivation assay
|
[PMID: 19783444] |
| HepG2 | EC50 |
50 nM
Compound: Rosiglitazone
|
Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
Transactivation of human PPARgamma expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay
|
[PMID: 21450468] |
| HepG2 | EC50 |
10 nM
Compound: Rosiglitazone
|
Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay
Agonist activity at PPARgamma receptor expressed in human HepG2 cells by PPRE-luciferase reporter gene assay
|
[PMID: 21482446] |
| HepG2 | EC50 |
0.02 μM
Compound: Rosi
|
Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
Agonist activity at human GAL4-fused PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay
|
[PMID: 22081932] |
| HepG2 | EC50 |
0.043 μg/mL
Compound: Rosiglitazone
|
Activation of PPAR in human HepG2 cells after 24 hrs by luciferase reporter gene assay
Activation of PPAR in human HepG2 cells after 24 hrs by luciferase reporter gene assay
|
[PMID: 22364952] |
| HepG2 | EC50 |
100 nM
Compound: Rosiglitazone
|
Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay
Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells by luciferase reporter gene assay
|
[PMID: 22934537] |
| HepG2 | EC50 |
0.039 μM
Compound: rosiglitazone
|
Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay
|
[PMID: 23171045] |
| HepG2 | EC50 |
0.002 μM
Compound: Rosiglitazone
|
Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
Agonist activity at GAL4-fused PPARgamma M463A mutant (unknown origin) expressed in human HepG2 cells by transactivation assay
|
[PMID: 23502212] |
| HepG2 | EC50 |
0.01 μM
Compound: Rosiglitazone
|
Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay
Agonist activity at GAL4-fused PPARgamma (unknown origin) expressed in human HepG2 cells by transactivation assay
|
[PMID: 23502212] |
| HepG2 | EC50 |
1.6 μM
Compound: Rosiglitazone
|
Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay
Transactivation of PPAR transfected in human HepG2 cells after 20 hrs by PPAR-luciferase assay
|
[PMID: 25437304] |
| HepG2 | EC50 |
0.039 μM
Compound: Rosiglitazone
|
Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay
Agonist activity at human GAL4-PPARgamma ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay
|
[PMID: 25462281] |
| HepG2 | EC50 |
0.04 μM
Compound: Rosiglitazone
|
Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
Agonist activity at GAL4-DNA binding domain fused human PPARgamma ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay
|
[PMID: 25497132] |
| HepG2 | EC50 |
0.04 μM
Compound: Rosiglitazone
|
Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay
Transactivation of GAL4-tagged human PPARgamma LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay
|
[PMID: 30996794] |
| HT-29 | IC50 |
45 μM
Compound: rosiglitazone
|
Antiproliferative activity against human HT29 cell line
Antiproliferative activity against human HT29 cell line
|
[PMID: 16821769] |
| Huh-7 | EC50 |
0.22 μM
Compound: 1
|
Functional activity at human PPAR gamma in Huh7 cells by transactivation assay
Functional activity at human PPAR gamma in Huh7 cells by transactivation assay
|
[PMID: 16366601] |
| Huh-7 | EC50 |
0.22 μM
Compound: 1
|
Effect on PPAR gamma transactivation activity in Huh7 cells
Effect on PPAR gamma transactivation activity in Huh7 cells
|
[PMID: 16451087] |
| Huh-7 | EC50 |
0.22 μM
Compound: rosiglitazone
|
Activity at human PPAR gamma in Huh7 cells by transactivation assay
Activity at human PPAR gamma in Huh7 cells by transactivation assay
|
[PMID: 17034149] |
| HUVEC | IC50 |
1.1 μM
Compound: Rosiglitazone
|
Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using freshly i
Anti-inflammatory activity in HUVEC assessed as reduction in TNFalpha-stimulated neutrophil-HUVEC interactions by measuring decrease in mononuclear leukocyte to endothelial cells pretreated for 20 hrs before TNFalpha stimulation for 24 hrs using freshly i
|
[PMID: 31268307] |
| Keratinocyte | IC50 |
8 μM
Compound: rosiglitazone
|
Antiproliferative activity against human keratinocytes
Antiproliferative activity against human keratinocytes
|
[PMID: 16821769] |
| L6 | EC50 |
5 μM
Compound: rosiglitazone
|
Effect on fatty acid oxidation in rat L6 cells
Effect on fatty acid oxidation in rat L6 cells
|
[PMID: 17343371] |
| L6 | EC50 |
4.49 μM
Compound: Rosiglitazone
|
Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin
Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose after 24 hrs in presence of insulin
|
[PMID: 23992862] |
| L6 | IC50 |
4.8 μM
Compound: Rosi
|
Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis
Increase in 2-[3H]-deoxyglucose uptake in rat L6 cells after 16 hrs by scintillation counting analysis
|
[PMID: 24813738] |
| MCF7 | IC50 |
>50 μM
Compound: rosiglitazone
|
Antiproliferative activity against human MCF7 cell line
Antiproliferative activity against human MCF7 cell line
|
[PMID: 16821769] |
| MCF7 | EC50 |
87 nM
Compound: rosiglitazone
|
Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
Agonist activity at human PPARgamma transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay
|
[PMID: 26226490] |
| MDA-MB-231 | IC50 |
5.23 μM
Compound: Rosiglitazone
|
Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay
|
[PMID: 25278236] |
| MG-63 | EC50 |
11 nM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay
Agonist activity at human PPARgamma expressed in MG-63 cells by reporter gene-based transactivation assay
|
[PMID: 22225641] |
| MG-63 | EC50 |
11 nM
Compound: Rosiglitazone
|
Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay
Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assay
|
[PMID: 22727448] |
| NIH3T3 | EC50 |
0.32 μM
Compound: rosiglitazone
|
Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay
Activity at human PPAR gamma transfected in NIH3T3 cells by luciferase activity assay
|
[PMID: 16854085] |
| NIH3T3 | EC50 |
0.32 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay
Agonist activity at human PPARgamma expressed in NIH3T3 cells by GAL4 transactivation assay
|
[PMID: 17624777] |
| PC-3 | IC50 |
20.3 μM
Compound: Rosiglitazone
|
Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human PC3 cells assessed as growth inhibition after 48 hrs by MTT assay
|
[PMID: 24996143] |
| Platelet | IC50 |
5.7 mM
Compound: 1; Rosi
|
Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation
Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of ADP-induced platelet aggregation
|
[PMID: 30481687] |
| Platelet | IC50 |
6.4 mM
Compound: 1; Rosi
|
Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation
Antiplatelet activity in platelet rich plasma (unknown origin) assessed as inhibition of arachidonic acid-induced platelet aggregation
|
[PMID: 30481687] |
| RAW264.7 | IC50 |
17.5 μM
Compound: BRL-49653
|
Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells
Suppression of LPS/IFN-gamma-stimulated NO production in mouse RAW264.7 cells
|
[PMID: 18809325] |
| Sf21 | IC50 |
40 μM
Compound: Rosiglitazone
|
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| Sf21 | IC50 |
6.4 μM
Compound: Rosiglitazone
|
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
|
[PMID: 21965623] |
| U2OS | EC50 |
0.03 μM
Compound: rosiglitazone
|
Effect on PPARgamma transactivation activity in U2OS cells
Effect on PPARgamma transactivation activity in U2OS cells
|
[PMID: 16300944] |
| U2OS | EC50 |
0.02 μM
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma in U2OS cells by transactivation assay
Agonist activity at human PPARgamma in U2OS cells by transactivation assay
|
[PMID: 18329751] |
| U2OS | EC50 |
0.01 M
Compound: Rosiglitazone
|
Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay
Agonist activity at human PPARgamma in human U2OS cells by cell based transactivation assay
|
[PMID: 19423341] |
| U2OS | EC50 |
0.05 μM
Compound: rosiglitazone
|
Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay
Agonist activity at human PPARgamma expressed in U2OS cells by luciferase transactivation assay
|
[PMID: 19574056] |
| U2OS | IC50 |
5.1 μM
Compound: Rosiglitazone
|
Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method
Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method
|
[PMID: 31439379] |
| U2OS | EC50 |
259.42 nM
Compound: ROS
|
Transactivation of human PPARgamma transfected in U2OS cells co-tranfected with human RXR measured after 24 hrs by luciferase reporter assay
Transactivation of human PPARgamma transfected in U2OS cells co-tranfected with human RXR measured after 24 hrs by luciferase reporter assay
|
[PMID: 31629632] |
Rosiglitazone (0.1-10 μM, 72 h) results in pluripotent C3H10T1/2 stem cell differentiation to adipocytes[1].
Rosiglitazone (1 μM, 24 h) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons[3].
Rosiglitazone (1 μM, 24 h) protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner[3].
Rosiglitazone (0.01-100 μM, 15 min) inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity respectively[4].
Rosiglitazone (0.5-50 μM, 7 days) inhibits ovarian cancer cell proliferation[7].
Rosiglitazone (5 μM, 7 days) suppresses Olaparib (HY-10162) induced alterations of cellular senescence and promotes apoptosis in A2780 and SKOV3 cells[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:A2780 and SKOV3 cells
-
Concentration:0.5-50 μM
-
Incubation Time:1-7 days
-
Result:Inhibited cell proliferation in a time‑dependent and concentration‑dependent manner.
-
Cell Line:Hippocampal neurons
-
Concentration:1 μM
-
Incubation Time:24 h
-
Result:Increased NF-α1 and BCL-2 protein level.
Rosiglitazone (intraperitoneal injection, 3 mg/kg/day) ameliorates airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα in male Wistar rats[6].
Rosiglitazone (intraperitoneal injection, 10 mg/kg, once every 2 days) inhibits subcutaneous ovarian cancer growth in A2780 and SKOV3 mouse subcutaneous xenograft models[7].
Rosiglitazone can exert neuroactive effects after intraperitoneal injection and modulate astrocyte polarization and neuroinflammation in a PPAR-γ dependent manner following experimental traumatic brain injury[8].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Streptozotocin (STZ)-induced diabetic rats[5]
-
Dosage:5 mg/kg
-
Administration:Oral administration, daily for 8 weeks.
-
Result:Decreased IL-6, TNF-α, and VCAM-1 levels in diabetic group.
Displayed lower levels of lipid peroxidation and NOx with an increase in aortic GSH and SOD levels compared to diabetic groups.
-
Animal Model:Male Wistar rats[6]
-
Dosage:3 mg/kg/day
-
Administration:Intraperitoneal injection, twice a day, 6 days per week for 12 consecutive weeks
-
Result:Ameliorated emphysema, elevated PEF, and higher level of total cells, neutrophils and cytokines (TNF-α and IL-1β) induced by cigarette smoke (CS).
Inhibited CS-induced M1 macrophage polarization and decreased the ratio of M1/M2.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 122320-73-4
-
Appearance Solid
-
분자량 357.43
-
화학식 C18H19N3O3S
-
Color White to off-white
-
SMILES
O=C(N1)SC(CC2=CC=C(OCCN(C)C3=NC=CC=C3)C=C2)C1=O
-
Synonyms
BRL 49653
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (189)
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Journal Impact Factor
-
Most Recent
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Cancer Cell
Tumor cell-intrinsic epigenetic dysregulation shapes cancer-associated fibroblasts heterogeneity to metabolically support pancreatic cancer. [Abstract]2024 May 13;42(5):869-884.e9. PMID: 38579725 -
Cell
2026 Jun 11;189(12):3571-3588.e27. PMID: 42019490 -
Cell
2026 May 28;189(11):3287-3305.e25. PMID: 42054994 -
Circulation
Cannabinoid Receptor 2-Centric Molecular Feedback Loop Drives Necroptosis in Diabetic Heart Injuries. [Abstract]2023 Jan 10;147(2):158-174. PMID: 36448459 -
Cell Metab
Microbial metabolite FAD mobilizes adipocyte lipid remodeling to enhance cancer immunotherapy efficacy. [Abstract]2026 Mar 3;38(3):565-581.e5. PMID: 41570815 -
Cell Metab
2023 Dec 5;35(12):2165-2182.e7. PMID: 38056430
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Cell Metab. 2023 Dec 5;35(12):2165-2182.e7. [Abstract]
Relative GDF15 mRNA expression and GDF15 release in human primary hepatocytes treated with 10 μM rosiglitazone for 48 h.
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Cell Metab
Bone marrow immune cells respond to fluctuating nutritional stress to constrain weight regain. [Abstract]2023 Nov 7;35(11):1915-1930.e8. PMID: 37703873
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Cell Metab. 2023 Nov 7;35(11):1915-1930.e8. [Abstract]
C3H10T1/2 preadipocytes were treated with differentiation medium supplemented with 0.5 mM 3-isobutyl-1-methylxanthine, 1 μM Dexamethasone, 850 nM Insulin, 1 nM Triiodothyronine, 125 nm Indomethacin and 1 μM Rosiglitazone for 2 days and subsequently cultured in maintaining medium supplemented with 1 nM Triiodothyronine, 850 nM Insulin, and 1 μM Rosiglitazone for another 2 days. Differentiated adipocytes at day 4 were cultured in complete medium until used for experiments. Representative immunoblots of PGC-1α and UCP1 in beige adipocytes treated as indicated.
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Cell Metab
2021 Mar 2;33(3):581-597.e9. PMID: 33440166
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Cell Metab. 2021 Mar 2;33(3):581-597.e9. [Abstract]
Protein expression of PPRC1 and PPARG in HepG2 cells exposed to PA and treated with RGZ (Rosiglitazone) (30 mmol/L; 24 h), as analyzed by western blot.
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Cancer Res
Disrupting Circadian Rhythm via the PER1-HK2 Axis Reverses Trastuzumab Resistance in Gastric Cancer. [Abstract]2022 Apr 15;82(8):1503-1517. PMID: 35255118 -
Nat Commun
Modulating the PPARγ pathway upregulates NECTIN4 and enhances chimeric antigen receptor (CAR) T cell therapy in bladder cancer. [Abstract]2025 Sep 10;16(1):8215. PMID: 40931013
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Sep 10;16(1):8215. [Abstract]
NECTIN4 mRNA levels in RT112 cells treated with 1μM Rosiglitazone and T0070907 (T007) for 72 h.
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Nat Commun
Senescent immune cells accumulation promotes brown adipose tissue dysfunction during aging. [Abstract]2023 Jun 2;14(1):3208. PMID: 37268694
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Jun 2;14(1):3208. [Abstract]
C3H10T1/2 preadipocytes were cultured in DMEM supplemented with 10% FBS, 1% P/S. For adipogenic differentiation, confluent C3H10T1/2 preadipocytes were incubated with complete medium supplemented with 0.5 mM 3-isobutyl-1-methylxanthine, 1 μM Dexamethasone, 850 nM Insulin, 1 nm Triiodothyronine, 125 nm Indomethacin and 1 μM Rosiglitazone for 2 days. Then, cells were changed to the complete medium supplemented with 1 nM T3, 850 nM Insulin, and 1 μM Rosiglitazone for another 2 days. Differentiated adipocytes at day 4 were maintained in complete medium until used for experiments. Representative immunoblots of NRP1 and EPHA7 in differentiated brown adipocytes transfected with si-Rbm3 or si-NC.
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Nat Commun
Peripheral modulation of antidepressant targets MAO-B and GABAAR by harmol induces mitohormesis and delays aging in preclinical models. [Abstract]2023 May 15;14(1):2779. PMID: 37188705 -
Metabolism
Prevention of insulin-induced lipohypertrophy by coadministration of a low dose of high-affinity PI3K inhibitors. [Abstract]2025 Mar 30:156252. PMID: 40169086 -
Redox Biol
Accumulated cholesterol protects tumours from elevated lipid peroxidation in the microenvironment. [Abstract]2023 Jun:62:102678. PMID: 36940607 -
J Nanobiotechnology
Suppression of senescent metabolism of adipose tissue by rebalancing mitochondrial homeostasis via a selective drug delivery system. [Abstract]2026 Jun 2. PMID: 42231423 -
Nucleic Acids Res
PPARG-centric transcriptional re-wiring during differentiation of human trophoblast stem cells into extravillous trophoblasts. [Abstract]2025 Jul 19;53(14):gkaf669. PMID: 40705926 -
J Nanobiotechnology
CT-sensitized nanoprobe for effective early diagnosis and treatment of pulmonary fibrosis. [Abstract]2025 Jan 29;23(1):60. PMID: 39881299 -
Theranostics
SOX4 promotes beige adipocyte-mediated adaptive thermogenesis by facilitating PRDM16-PPARγ complex. [Abstract]2022 Nov 7;12(18):7699-7716. PMID: 36451857 -
Theranostics
The peroxisome proliferator-activated receptor agonist rosiglitazone specifically represses tumour metastatic potential in chromatin inaccessibility-mediated FABP4-deficient gastric cancer. [Abstract]2022 Jan 24;12(4):1904-1920. PMID: 35198079 -
Acta Pharm Sin B
2025 Dec;15(12):6382-6398. PMID: 41477334 -
J Biomed Sci
USP24 upregulation stabilizes PKA-Cα to promote lipogenesis, inflammation, and fibrosis during MASH progression. [Abstract]2025 May 30;32(1):54. PMID: 40448065 -
J Exp Clin Cancer Res
SNAI1 promotes epithelial-mesenchymal transition and maintains cancer stem cell-like properties in thymic epithelial tumors through the PIK3R2/p-EphA2 Axis. [Abstract]2024 Dec 19;43(1):324. PMID: 39702326 -
Adv Sci (Weinh)
Cars2-Mediated Cysteine Catabolism Drives Brown Fat Development and Thermogenesis Through Persulfidating EBF2. [Abstract]2026 Mar 18:e22690. PMID: 41849685 -
Adv Sci (Weinh)
SR-B1-Mediated Transplacental Transfer of Hydrophobic Toxicants Disrupts Fetal Development During Barriergenesis. [Abstract]2026 Apr;13(23):e15742. PMID: 41736660 -
Adv Sci (Weinh)
FGF2 Mediated USP42-PPARγ Axis Activation Ameliorates Liver Oxidative Damage and Promotes Regeneration. [Abstract]2025 May;12(18):e2408724. PMID: 40091484 -
Adv Sci (Weinh)
Photothermal-Responsive Soluble Microneedle Patches for Meibomian Gland Dysfunction Therapy. [Abstract]2025 Jan 30:e2413962. PMID: 39887671 -
Adv Sci (Weinh)
Inhibition of CDK1 Overcomes Oxaliplatin Resistance by Regulating ACSL4-mediated Ferroptosis in Colorectal Cancer. [Abstract]2023 Sep;10(25):e2301088. PMID: 37428466 -
Cell Death Differ
Epigenetic regulation of ACSL4 via H2A monoubiquitylation connects lipid metabolism to BAP1-mediated ferroptosis. [Abstract]2025 Nov 27. PMID: 41310183 -
Cell Death Differ
Blockage of PPARγ T166 phosphorylation enhances the inducibility of beige adipocytes and improves metabolic dysfunctions. [Abstract]2023 Mar;30(3):766-778. PMID: 36329235 -
Cardiovasc Res
METTL14 inhibits atherogenesis by epigenetically activating PPAR-α/γ transcription and fatty acid oxidation in VSMCs. [Abstract]2026 Mar 24:cvag069. PMID: 41873711 -
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J Control Release
Metabolism-modulating nanoparticles for remodeling adipose-liver crosstalk to reverse liver fibrosis. [Abstract]2026 May 15:115026. PMID: 42142745 -
Cell Death Dis
ACSL4-mediated lipid rafts prevent membrane rupture and inhibit immunogenic cell death in melanoma. [Abstract]2024 Sep 29;15(9):695. PMID: 39343834 -
Cell Death Dis
Seipin deficiency-induced lipid dysregulation leads to hypomyelination-associated cognitive deficits via compromising oligodendrocyte precursor cell differentiation. [Abstract]2024 May 21;15(5):350. PMID: 38773070 -
Cell Death Dis
Gp78 deficiency in hepatocytes alleviates hepatic ischemia-reperfusion injury via suppressing ACSL4-mediated ferroptosis. [Abstract]2023 Dec 8;14(12):810. PMID: 38065978 -
Cell Death Dis
2023 Apr 6;14(4):246. PMID: 37024456 -
Cell Mol Biol Lett
2022 Feb 2;27(1):11. PMID: 35109789 -
Pharmacol Res
A novel FFA1 agonist, CPU025, improves glucose-lipid metabolism and alleviates fatty liver in obese-diabetic (ob/ob) mice. [Abstract]2020 Mar;153:104679. PMID: 32014571 -
Cell Commun Signal
Identification of novel SCD1 inhibitor alleviates nonalcoholic fatty liver disease: critical role of liver-adipose axis. [Abstract]2023 Sep 30;21(1):268. PMID: 37777801 -
J Exp Med
Intermittent prednisone treatment in mice promotes exercise tolerance in obesity through adiponectin. [Abstract]2022 May 2;219(5):e20211906. PMID: 35363257 -
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Phytomedicine
Perillyl alcohol ameliorates high-fat diet-induced obesity in mice by modulating gut microbiota and activating IRF4-mediated brown fat thermogenesis. [Abstract]2025 Oct 11:148:157400. PMID: 41138577 -
EBioMedicine
PPAR-γ suppresses macrophage senescence and allergic airway inflammation through controlling lipid metabolic pathways. [Abstract]2026 Apr:126:106226. PMID: 41864062 -
J Pharm Anal
1,8-Cineole ameliorates vascular endothelial senescence in diabetes mellitus by directly targeting and deubiquitinating PPAR-γ in vivo and in vitro. [Abstract]2025 Dec;15(12):101307. PMID: 41492461 -
J Pharm Anal
Effect of cholesterol on distribution, cell uptake, and protein corona of lipid microspheres at sites of cardiovascular inflammatory injury. [Abstract]2025 Jul;15(7):101182. PMID: 40735031 -
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J Hazard Mater
Underlying mechanisms of metabolic dysfunction-associated steatotic liver disease induced by 2-ethylhexyl diphenyl phosphate and its hydroxylated metabolite in zebrafish (Danio rerio). [Abstract]2025 Apr 24:493:138407. PMID: 40300519 -
Acta Pharmacol Sin
Few-shot learning-driven discovery of Lutein suppresses Th1-mediated inflammation via glucose metabolism. [Abstract]2026 May 18. PMID: 42144445 -
Cell Death Discov
DNMBP-AS1/hsa-miR-30a-5p/PGC1α axis suppresses tumor progression of colorectal cancer by inhibiting PKM2-mediated Warburg effect and enhance anti-PD-1 therapy efficacy. [Abstract]2025 Jul 2;11(1):299. PMID: 40603870 -
Acta Pharmacol Sin
Fisetin treatment alleviates kidney injury in mice with diabetes-exacerbated atherosclerosis through inhibiting CD36/fibrosis pathway. [Abstract]2023 Oct;44(10):2065-2074. PMID: 37225845 -
Cell Death Discov
Disturbance of calcium homeostasis and myogenesis caused by TET2 deletion in muscle stem cells. [Abstract]2022 Apr 30;8(1):236. PMID: 35490157 -
Environ Int
Adipogenic and osteogenic effects of OBS and synergistic action with PFOS via PPARγ-RXRα heterodimers. [Abstract]2024 Jan:183:108354. PMID: 38043320 -
J Orthop Translat
Semaglutide alleviates osteoarthritis independent of weight loss via GLP-1R-mediated activation of autophagy through AKT/mTOR inhibition. [Abstract]2026 Jun 23;59:101166. PMID: 42381999 -
ACS Environ Au
Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]2025 Aug 5;5(6):573-582. PMID: 41277996 -
Int J Biol Macromol
2025 Dec 30;339(Pt 2):149976. PMID: 41478474 -
EMBO J
2025 Nov 20. PMID: 41266655 -
Mol Med
Elabela alleviates cuproptosis and vascular calcification in vitaminD3- overloaded mice via regulation of the PPAR-γ /FDX1 signaling. [Abstract]2024 Nov 20;30(1):223. PMID: 39567863 -
Antioxidants (Basel)
Ginsenoside Rg1 Alleviates Blood-Milk Barrier Disruption in Subclinical Bovine Mastitis by Regulating Oxidative Stress-Induced Excessive Autophagy. [Abstract]2024 Nov 24;13(12):1446. PMID: 39765775 -
Phytother Res
Pinoresinol Diglucoside Alleviates Cardiac Fibrosis Through Inhibiting Endothelial-Mesenchymal Transition via the Transforming Growth Factor-β1/Smads Pathway in db/db Mice. [Abstract]2025 Dec;39(12):5765-5776. PMID: 41188687 -
Phytother Res
Increasing brain glucose uptake by Gypenoside LXXV ameliorates cognitive deficits in a mouse model of diabetic Alzheimer's disease. [Abstract]2023 Feb;37(2):611-626. PMID: 36325883 -
Free Radic Biol Med
Thiomyristoyl promotes type 2 diabetic wound healing and inhibits scarring via the PPARγ/Sirt3/SOD2 axis. [Abstract]2026 Jun 8:254:31-45. PMID: 42264197 -
Free Radic Biol Med
2018 Oct:126:259-268. PMID: 30138713
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2018 Oct:126:259-268. [Abstract]
Laser confocal microscope is performed to measure MMP indicated with the ratio of JC-1 Red/JC-1 Green. Nuclei are counterstained with DAPI (blue). Bar graphs represent the mean ± SD of red/green fluorescence intensity.
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Stem Cell Res Ther
MSCs promote the efferocytosis of large peritoneal macrophages to eliminate ferroptotic monocytes/macrophages in the injured endometria. [Abstract]2024 May 1;15(1):127. PMID: 38693589 -
Cell Rep
NAD+ sensing by PARP7 regulates the C/EBPβ-dependent transcription program during adipogenesis. [Abstract]2026 Jan 30;45(2):116929. PMID: 41621069 -
Cell Rep
Paracrine stimulation of brown adipose tissue vascularization by adipocyte O-GlcNAc signaling. [Abstract]2025 Dec 11;44(12):116678. PMID: 41385373 -
Cell Rep
Blocking glycogen synthase 1 in white adipose tissue alleviates hypermetabolism following severe burn injury through inhibition of JAK2 by UDPG. [Abstract]2025 Nov 18;44(12):116577. PMID: 41259203 -
Cell Rep
Exercise-induced adipokine Nrg4 alleviates MASLD by disrupting hepatic cGAS-STING signaling. [Abstract]2025 Jan 30;44(2):115251. PMID: 39891907 -
Cell Prolif
Decreased YB-1 expression denervates brown adipose tissue and contributes to age-related metabolic dysfunction. [Abstract]2024 Jan;57(1):e13520. PMID: 37321837 -
Br J Pharmacol
HWL-088, a new potent free fatty acid receptor 1 (FFAR1) agonist, improves glucolipid metabolism and acts additively with metformin in ob/ob diabetic mice. [Abstract]2020 May;177(10):2286-2302. PMID: 31971610 -
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Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
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Cancer Cell Int
Enhancing prognostic accuracy in head and neck squamous cell carcinoma chemotherapy via a lipid metabolism-related clustered polygenic model. [Abstract]2023 Aug 11;23(1):164. PMID: 37568192 -
J Ethnopharmacol
Euphorbia humifusa Willd. alleviates ulcerative colitis by inhibiting lipid peroxidation via ACSL4/COX-2 axis. [Abstract]2026 Sep 15:368:121839. PMID: 42106018 -
J Ethnopharmacol
Essential oil from Fructus Alpiniae zerumbet ameliorates vascular endothelial cell senescence in diabetes by regulating PPAR-γ signalling: A 4D label-free quantitative proteomics and network pharmacology study. [Abstract]2024 Mar 1:321:117550. PMID: 38065350 -
Eur J Med Chem
Design, synthesis and anti-diabetic evaluation of novel PPAR agonists based on functional group-oriented strategy. [Abstract]2025 Oct 9:301:118226. PMID: 41075607 -
Eur J Med Chem
Design, synthesis, and biological evaluation of imidazolidinone derivatives as potent PPARα/δ agonists for the treatment of cholestatic liver diseases. [Abstract]2025 Jan 15:286:117284. PMID: 39827490 -
Eur J Med Chem
Discovery of new and highly effective quadruple FFA1 and PPARα/γ/δ agonists as potential anti-fatty liver agents. [Abstract]2022 Feb 5:229:114061. PMID: 34954593 -
Eur J Med Chem
Discovery of the first-in-class dual PPARδ/γ partial agonist for the treatment of metabolic syndrome. [Abstract]2021 Dec 5:225:113807. PMID: 34455359 -
Ecotoxicol Environ Saf
PPARγ-responsive luciferase reporter system for high-throughput screening of chemical toxins with potential pulmonary fibrosis effects. [Abstract]2025 Nov 15:307:119433. PMID: 41273832 -
Ecotoxicol Environ Saf
Effects of benzotriazoles UV-328, UV-329, and UV-P on the self-renewal and adipo-osteogenic differentiation of human mesenchymal stem cells. [Abstract]2025 Jan 22:290:117765. PMID: 39847882 -
CNS Neurosci Ther
The Neuroprotective Mechanisms of PPAR-γ: Inhibition of Microglia-Mediated Neuroinflammation and Oxidative Stress in a Neonatal Mouse Model of Hypoxic-Ischemic White Matter Injury. [Abstract]2024 Nov;30(11):e70081. PMID: 39496476 -
Ocul Surf
2024 Oct:34:444-458. PMID: 39395739 -
Ecotoxicol Environ Saf
Excessive selenium affects neural development and locomotor behavior of zebrafish embryos. [Abstract]2022 Jun 15;238:113611. PMID: 35526456 -
Cell Mol Life Sci
Myogenic enhancer snatching promotes adipogenic differentiation during epigenetic reprogramming mediated by lineage-specific transcription factors. [Abstract]2025 Nov 19;82(1):412. PMID: 41258103 -
Life Sci
Combination therapy with semaglutide and rosiglitazone as a synergistic treatment for diabetic retinopathy in rodent animals. [Abstract]2021 Mar 15:269:119013. PMID: 33417950 -
Compr Physiol
The Acyltransferase Transmembrane Protein 68 Promotes Neutral Lipid Storage in Mouse Adipocytes. [Abstract]2026 Jun;16(3):e70175. PMID: 42148591 -
Biomed J
Inhibition of the 4-hydroxynonenal-regulated JNK/c-Jun pathway improves bleomycin-induced lung fibrosis. [Abstract]2025 Oct 9:100916. PMID: 41076274 -
Mol Metab
RNA-binding protein YBX3 promotes PPARγ-SLC3A2 mediated BCAA metabolism fueling brown adipogenesis and thermogenesis. [Abstract]2024 Oct 29:102053. PMID: 39481849 -
Food Funct
Curcumin inhibits cigarette smoke-induced inflammation via modulating the PPARγ-NF-κB signaling pathway. [Abstract]2019 Dec 11;10(12):7983-7994. PMID: 31773117 -
Inflamm Res
Rosiglitazone attenuates Acute Kidney Injury from hepatic ischemia-reperfusion in mice by inhibiting arachidonic acid metabolism through the PPAR-γ/NF-κB pathway. [Abstract]2024 Oct;73(10):1765-1780. PMID: 39112648 -
Cells
Oleic Acid and Transferrin Synergistically Induce Serum-Free Adipogenic Differentiation of Porcine Preadipocytes via the SEPTIN4/PPARγ Axis. [Abstract]2026 Apr 13;15(8):684. PMID: 42041552 -
Cells
The Asp-Encoding Gene FBN1 Mediates Cold Adaptation in Sunite Sheep by Reprogramming Adipocyte Differentiation Towards Thermogenesis. [Abstract]2026 Feb 11;15(4):329. PMID: 41744772 -
Cells
2021 Dec 28;11(1):86. PMID: 35011648 -
Nutrients
Medium-Chain Fatty Acids Selectively Sensitize Cancer Cells to Ferroptosis by Inducing CD36 and ACSL4. [Abstract]2025 Feb 25;17(5):794. PMID: 40077664 -
Commun Biol
PPARγ alleviates preeclampsia development by regulating lipid metabolism and ferroptosis. [Abstract]2024 Apr 9;7(1):429. PMID: 38594496 -
Eur J Pharmacol
The therapeutic potential of Rosiglitazone in modulating scar formation through PPAR-γ pathway. [Abstract]2025 Jun 5:996:177445. PMID: 40054722 -
Eur J Pharmacol
GW9662 ameliorates nonalcoholic steatohepatitis by inhibiting the PPARγ/CD36 pathway and altering the gut microbiota. [Abstract]2023 Dec 5:960:176113. PMID: 37838102 -
Pharmaceuticals (Basel)
Rosiglitazone Does Not Show Major Hidden Cardiotoxicity in Models of Ischemia/Reperfusion but Abolishes Ischemic Preconditioning-Induced Antiarrhythmic Effects in Rats In Vivo. [Abstract]2022 Aug 26;15(9):1055. PMID: 36145276 -
Eur J Pharmacol
Proteomic analysis reveals that ACSL4 activation during reflux esophagitis contributes to ferroptosis-mediated esophageal mucosal damage. [Abstract]2022 Sep 15:931:175175. PMID: 35921957 -
J Zhejiang Univ Sci B
Silencing of DsbA-L gene impairs the PPARγ agonist function of improving insulin resistance in a high-glucose cell model. [Abstract]2020;21(12):990-998. PMID: 33843164 -
Eur J Pharmacol
Hepatoprotective effects of ZLY16, a dual peroxisome proliferator-activated receptor α/δ agonist, in rodent model of nonalcoholic steatohepatitis. [Abstract]2020 Sep 5;882:173300. PMID: 32592770 -
Eur J Pharmacol
MicroRNA-128 knockout inhibits the development of Alzheimer's disease by targeting PPARγ in mouse models. [Abstract]2019 Jan 15:843:134-144. PMID: 30412727
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 Jan 15:843:134-144. [Abstract]
Protein levels of BACE1 and APP are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 Jan 15:843:134-144. [Abstract]
Protein levels of sAPPα and sAPPβ are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2019 Jan 15:843:134-144. [Abstract]
PPARγ level is determined by IF assay in 3×Tg-AD mice, 3×Tg-AD mice with RSG treatment, 3×Tg-AD-KO mice, 3×Tg-AD-KO mice with GW9662 stimulation.
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Int J Mol Sci
Establishment and Comparative Analysis of Four Mouse Models for the Study of Pancreatic Steatosis. [Abstract]2026 May 10;27(10):4255. PMID: 42196238 -
Int Immunopharmacol
Trem2 prevents adverse pregnancy outcomes induced by Toxoplasma gondii by promoting PPARγ-mediated P-STAT6 signaling. [Abstract]2026 Jan 1;168(Pt 1):115739. PMID: 41175738 -
Int J Mol Sci
2025 Oct 18;26(20):10132. PMID: 41155424 -
Int J Mol Sci
Inhibition of ACSL4 Attenuates Behavioral Deficits by Regulating Ferroptosis in a Murine Model of Systemic Lupus Erythematosus. [Abstract]2025 Apr 10;26(8):3553. PMID: 40332005 -
Int Immunopharmacol
LncRNA SNHG7 alleviates IL-1β-induced osteoarthritis by inhibiting miR-214-5p-mediated PPARGC1B signaling pathways. [Abstract]2021 Jan;90:107150. PMID: 33296783 -
Am J Physiol Cell Physiol
2026 Jan 1;330(1):C142-C154. PMID: 41269663 -
Front Pharmacol
Metformin Attenuates Cardiac Hypertrophy Via the HIF-1α/PPAR-γ Signaling Pathway in High-Fat Diet Rats. [Abstract]2022 Jun 27;13:919202. PMID: 35833024 -
Front Cell Dev Biol
2020 Jul 29;8:703. PMID: 32850823 -
Bioorg Chem
Discovery of Tetrazolone derivatives as potent PPARα/δ dual agonists for metabolic dysfunction-associated steatohepatitis. [Abstract]2026 Jul 5:175:109764. PMID: 41880786 -
Molecules
Identification of Novel PPARγ Partial Agonists Based on Virtual Screening Strategy: In Silico and In Vitro Experimental Validation. [Abstract]2024 Oct 15;29(20):4881. PMID: 39459249 -
Bioorg Chem
Structure-based screening and biological validation of the anti-thrombotic drug-dicoumarol as a novel and potent PPARγ-modulating ligand. [Abstract]2022 Dec:129:106191. PMID: 36270169 -
J Physiol Biochem
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Front Mol Biosci
2022 Feb 4;8:766887. PMID: 35187064 -
Front Mol Neurosci
Rosiglitazone Exerts an Anti-depressive Effect in Unpredictable Chronic Mild-Stress-Induced Depressive Mice by Maintaining Essential Neuron Autophagy and Inhibiting Excessive Astrocytic Apoptosis. [Abstract]2017 Sep 14;10:293. PMID: 28959186
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Front Mol Neurosci. 2017 Sep 14;10:293. [Abstract]
Rosiglitazone enhances the phosphorylation of insulin receptor substrate 1 (IRS1, phosphorylated at Ser 636/639), which is considered to be the main activator of the Akt/mTOR pathway by IGF-1R.
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Front Physiol
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Am J Physiol Endocrinol Metab
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PPARγ/Adiponectin axis attenuates methamphetamine-induced conditional place preference via the hippocampal AdipoR1 signaling pathway. [Abstract]2023 Jul 13:125:110758. PMID: 36972780 -
Clin Immunol
Elevated asprosin expression exacerbates synovial inflammation by PPAR-γ-dependent mechanisms in rheumatoid arthritis. [Abstract]2026 Apr:284:110677. PMID: 41638328 -
J Biol Chem
PPARγ and C/EBPα enable adipocyte differentiation upon inhibition of histone methyltransferase PRC2 in malignant tumors. [Abstract]2024 Sep 12:107765. PMID: 39276936 -
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Neuromolecular Med
Seipin Deficiency Impairs Motor Coordination in Mice by Compromising Spinal Cord Myelination. [Abstract]2025 Jan 27;27(1):12. PMID: 39869141 -
Carcinogenesis
ACSL4: a Double-edged Sword Target in Multiple Myeloma, Promotes Cell Proliferation and Sensitizes Cell to Ferroptosis. [Abstract]2023 May 27;44(3):242-251. PMID: 36999754
Rosiglitazone purchased from MedChemExpress. Usage Cited in: Carcinogenesis. 2023 May 27;44(3):242-251. [Abstract]
Rosiglitazone (ROSI; 15, 30, 60, 120, 240 µM; 24 h) significantly inhibits the growth of NCI-H929 and OPM-2 cells.
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Ren Fail
Rosiglitazone attenuates hypoxia-induced renal cell apoptosis by inhibiting NF-κB signaling pathway in a PPARγ-dependent manner. [Abstract]2022 Dec;44(1):2056-2065. PMID: 36420656 -
Biochim Biophys Acta Mol Cell Biol Lipids
Regulation of adiponectin on lipid metabolism in large yellow croaker (Larimichthys crocea). [Abstract]2020 Aug;1865(8):158711. PMID: 32289502 -
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Exp Cell Res
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Agarotetrol attenuates spinal cord injury by targeting PPARγ to modulate microglial activation. [Abstract]2026 May 1;458(1):114947. PMID: 41720447 -
Bioorg Med Chem
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Sci Total Environ
UV filter ethylhexyl salicylate affects cardiovascular development by disrupting lipid metabolism in zebrafish embryos. [Abstract]2023 Aug 25:888:164073. PMID: 37201812 -
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용액&용해도
DMSO : 175 mg/mL (489.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : 2 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)
H2O : < 0.1 mg/mL (insoluble)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.99 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.99 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 10 mg/mL (27.98 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6. [Content Brief]
[2]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8. [Content Brief]
[3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70. [Content Brief]
[4]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30. [Content Brief]
[5]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220. [Content Brief]
[6]. Haoshen Feng, et al. Rosiglitazone ameliorated airway inflammation induced by cigarette smoke via inhibiting the M1 macrophage polarization by activating PPARγ and RXRα. Int Immunopharmacol. 2021 Aug;97:107809. [Content Brief]
[7]. Zehua Wang, et al. Rosiglitazone ameliorates senescence and promotes apoptosis in ovarian cancer induced by olaparib. Cancer Chemother Pharmacol. 2020 Feb;85(2):273-284. [Content Brief]
[8]. Ren X, et al. Rosiglitazone regulates astrocyte polarization and neuroinflammation in a PPAR-γ dependent manner after experimental traumatic brain injury. Brain Res Bull. 2024 Apr;209:110918. [Content Brief]
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. 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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.7978 mL | 13.9888 mL | 27.9775 mL | 69.9438 mL |
| 5 mM | 0.5596 mL | 2.7978 mL | 5.5955 mL | 13.9888 mL | |
| DMSO | 10 mM | 0.2798 mL | 1.3989 mL | 2.7978 mL | 6.9944 mL |
| 15 mM | 0.1865 mL | 0.9326 mL | 1.8652 mL | 4.6629 mL | |
| 20 mM | 0.1399 mL | 0.6994 mL | 1.3989 mL | 3.4972 mL | |
| 25 mM | 0.1119 mL | 0.5596 mL | 1.1191 mL | 2.7978 mL | |
| 30 mM | 0.0933 mL | 0.4663 mL | 0.9326 mL | 2.3315 mL | |
| 40 mM | 0.0699 mL | 0.3497 mL | 0.6994 mL | 1.7486 mL | |
| 50 mM | 0.0560 mL | 0.2798 mL | 0.5596 mL | 1.3989 mL | |
| 60 mM | 0.0466 mL | 0.2331 mL | 0.4663 mL | 1.1657 mL | |
| 80 mM | 0.0350 mL | 0.1749 mL | 0.3497 mL | 0.8743 mL | |
| 100 mM | 0.0280 mL | 0.1399 mL | 0.2798 mL | 0.6994 mL |