Art. -Nr.: HY-17386

Rosiglitazone

(Synonyms: BRL 49653)

176 Cited Publications

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Based on 176 publication(s) in Google Scholar

Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 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.

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Reinheit: 99.94%
CAS. Nr.: 122320-73-4
Formel: C₁₈H₁₉N₃O₃S
Molecular Weight:357.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Rosiglitazone Chemical Structure

CAS. Nr.: 122320-73-4

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (176)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]^[4]

PPARγ

40 nM (Kd)

PPARγ

60 nM (EC₅₀)

TRPC5

30 μM (EC₅₀)

TRPM3

Alle PPAR Isoform-spezifische Produkte anzeigen :

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

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]

In Vitro

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 Proliferation Assay^[7]

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.

Western Blot Analysis^[3]

Cell Line:

Hippocampal neurons
Concentration:

1 μM
Incubation Time:

24 h
Result:

Increased NF-α1 and BCL-2 protein level.

In Vivo

Rosiglitazone (oral administration, 5 mg/kg, daily for 8 weeks) decreases the serum glucose in diabetic rats^[5].
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 122320-73-4
Appearance Solid
Molecular Weight 357.43
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (176)

All WBRT-PCRIFCell Proliferation/Viability Assay

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Journal Impact Factor

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

Unbiased niche labeling maps immune-excluded niche in bone metastasis. [Abstract]

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

GDF15 is a major determinant of ketogenic diet-induced weight loss. [Abstract]

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.
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.
Cell Metab

An isocaloric moderately high-fat diet extends lifespan in male rats and Drosophila. [Abstract]

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.
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.
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.
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
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
Acta Pharm Sin B

Generation and applications of an expandable and mature hiPSC-derived liver organoid. [Abstract]

2025 Dec;15(12):6382-6398. PMID: 41477334
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
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
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
Chem Eng J

2025 Oct 17;524:169708.
Chem Eng J

2023 Aug 6, 145212.
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 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
J Nanobiotechnology

CT-sensitized nanoprobe for effective early diagnosis and treatment of pulmonary fibrosis. [Abstract]

2025 Jan 29;23(1):60. PMID: 39881299
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
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 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
EBioMedicine

PPAR-γ suppresses macrophage senescence and allergic airway inflammation through controlling lipid metabolic pathways. [Abstract]

2026 Apr:126:106226. PMID: 41864062
J Exp Med

Intermittent prednisone treatment in mice promotes exercise tolerance in obesity through adiponectin. [Abstract]

2022 May 2;219(5):e20211906. PMID: 35363257
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 Mol Biol Lett

Slc25a5 regulates adipogenesis by modulating ERK signaling in OP9 cells. [Abstract]

2022 Feb 2;27(1):11. PMID: 35109789
Environ Int

Adipogenic and osteogenic effects of OBS and synergistic action with PFOS via PPARγ-RXRα heterodimers. [Abstract]

2024 Jan:183:108354. PMID: 38043320
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

Melatonin inhibits bladder tumorigenesis by suppressing PPARγ/ENO1-mediated glycolysis. [Abstract]

2023 Apr 6;14(4):246. PMID: 37024456
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
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
Int J Biol Macromol

Rbbp7-mediated deacetylation of Acsl4 promotes ovarian aging by enhancing ferroptosis. [Abstract]

2025 Dec 30;339(Pt 2):149976. PMID: 41478474
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
Phytomedicine

2025 Dec 28.
EMBO J

The NLRP6 inflammasome is activated by sterile or pathogen-induced endolysosomal damage. [Abstract]

2025 Nov 20. PMID: 41266655
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
Free Radic Biol Med

TRPM2 mediates mitochondria-dependent apoptosis of melanocytes under oxidative stress. [Abstract]

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.
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
Sci Total Environ

Antibiotics disrupt lipid metabolism in zebrafish (Danio rerio) larvae and 3T3-L1 preadipocytes. [Abstract]

2023 Feb 1;858(Pt 1):159755. PMID: 36349636
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
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
Biomed Pharmacother

Identification of a novel PPARγ modulator with good anti-diabetic therapeutic index via structure-based screening, optimization and biological validation. [Abstract]

2022 Oct:154:113653. PMID: 36942599
Biomed Pharmacother

PPARγ activation mitigates mechanical allodynia in paclitaxel-induced neuropathic pain via induction of Nrf2/HO-1 signaling pathway. [Abstract]

2020 Sep;129:110356. PMID: 32535388
Food Science and Human Wellness

2023 Nov;12(6);2061-2072.
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
Journal of Future Foods

2025 Jul 8.
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
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
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
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
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
Mol Metab

RNA-binding protein YBX3 promotes PPARγ-SLC3A2 mediated BCAA metabolism fueling brown adipogenesis and thermogenesis. [Abstract]

2024 Oct 29:102053. PMID: 39481849
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
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
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
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
Ecotoxicol Environ Saf

Excessive selenium affects neural development and locomotor behavior of zebrafish embryos. [Abstract]

2022 Jun 15;238:113611. PMID: 35526456
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
Environ Health

2026 Jan 26.
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
Ocul Surf

Cytarabine chemotherapy induces meibomian gland dysfunction. [Abstract]

2024 Oct:34:444-458. PMID: 39395739
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
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
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
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
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

PPARγ Regulates Triclosan Induced Placental Dysfunction. [Abstract]

2021 Dec 28;11(1):86. PMID: 35011648
Commun Biol

PPARγ alleviates preeclampsia development by regulating lipid metabolism and ferroptosis. [Abstract]

2024 Apr 9;7(1):429. PMID: 38594496
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
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
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
Int J Mol Sci

Rebamipide Induces Hair Regeneration Through EP4-Driven Lipid Metabolism Remodeling. [Abstract]

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
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
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
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
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
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
Am J Physiol Cell Physiol

Adipose tissue releases nucleosides. [Abstract]

2026 Jan 1;330(1):C142-C154. PMID: 41269663
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
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
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
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
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.
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
Biomed J

Inhibition of the 4-hydroxynonenal-regulated JNK/c-Jun pathway improves bleomycin-induced lung fibrosis. [Abstract]

2025 Oct 9:100916. PMID: 41076274
J Physiol Biochem

Blockage of NDUFB9-SCD1 pathway inhibits adipogenesis : Blockage of NDUFB9-SCD1 pathway inhibits adipogenesis. [Abstract]

2022 May;78(2):377-388. PMID: 35122619
Front Cell Dev Biol

Bergenin as a Novel Urate-Lowering Therapeutic Strategy for Hyperuricemia. [Abstract]

2020 Jul 29;8:703. PMID: 32850823
Poult Sci

Three alternative promoters govern PGC-1α expression in chicken and are directly repressed by PPARγ. [Abstract]

2026 Jan 18;105(4):106481. PMID: 41610606
Exp Neurol

RvD1 signaling in peripheral macrophages promotes systemic β-amyloid clearance to mitigate the progression of perioperative neurocognitive disorders in mice. [Abstract]

2025 Oct 11:395:115486. PMID: 41082997
Drug Dev Res

Tilianin alleviates lipid deposition and fibrosis in mice with nonalcoholic steatohepatitis by activating the PPARα/Nnat axis. [Abstract]

2023 Aug;84(5):922-936. PMID: 37052239
J Cell Mol Med

Hoxa5 alleviates obesity-induced chronic inflammation by reducing ER stress and promoting M2 macrophage polarization in mouse adipose tissue. [Abstract]

2019 Oct;23(10):7029-7042. PMID: 31441588
J Lipid Res

KLF7 induced ADRB3-dependent IL-6 production in brown adipocytes during stress. [Abstract]

2026 Feb;67(2):100981. PMID: 41565113
iScience

Patient-derived organoid xenografts model esophageal cancer cachexia and enable assessment of anti-inflammatory drug repositioning. [Abstract]

2026 Jan 7;29(2):114638. PMID: 41623495
iScience

Suppression of preadipocyte determination by SOX4 limits white adipocyte hyperplasia in obesity. [Abstract]

2023 Feb 28;26(4):106289. PMID: 36968079
iScience

Metabolic modeling of single bronchoalveolar macrophages reveals regulators of hyperinflammation in COVID-19. [Abstract]

2022 Oct 10;25(11):105319. PMID: 36246577
Front Mol Biosci

Down-Regulated miR-130a/b Attenuates Rhabdomyosarcoma Proliferation via PPARG. [Abstract]

2022 Feb 4;8:766887. PMID: 35187064
J Cell Physiol

PPARγ promotes diabetes-associated centrosome amplification via increasing the expression of SKA1 directly at the transcriptional level. [Abstract]

2019 Nov;234(11):20694-20703. PMID: 30989671
Aquaculture

2026 Jan 4;615:743618.
J Drug Target

Dual AMPK activation and TXNIP suppression underlie the superior anti-diabetic action of rosiglitazone-metformin co-crystal (RZM): evidence from preclinical models. [Abstract]

2025 Jul 17:1-10. PMID: 40658109
Neuromolecular Med

Seipin Deficiency Impairs Motor Coordination in Mice by Compromising Spinal Cord Myelination. [Abstract]

2025 Jan 27;27(1):12. PMID: 39869141
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
Sci Rep

The role of RUNX1/NF-κB in regulating PVAT inflammation in aortic dissection. [Abstract]

2024 Apr 30;14(1):9960. PMID: 38693222
Aquaculture

2024 Jan 15, 578, 740081.
Prog Neuropsychopharmacol Biol Psychiatry

PPARγ/Adiponectin axis attenuates methamphetamine-induced conditional place preference via the hippocampal AdipoR1 signaling pathway. [Abstract]

2023 Jul 13:125:110758. PMID: 36972780
Biomedicines

PFOS Inhibited Normal Functional Development of Placenta Cells via PPARγ Signaling. [Abstract]

2021 Jun 15;9(6):677. PMID: 34203907
Clin Immunol

Elevated asprosin expression exacerbates synovial inflammation by PPAR-γ-dependent mechanisms in rheumatoid arthritis. [Abstract]

2026 Apr:284:110677. PMID: 41638328
Food Sci Nutr

Anti-Diabetic Effects of Ayanin, a Flavonoid Compound, in STZ/HFD-Induced Diabetic Mice by Upregulating GLUT4 and Suppressing Macrophage-Driven Inflammation in Adipose Tissues. [Abstract]

2026 Jan 7;14(1):e71429. PMID: 41509193
Food Sci Nutr

Screening Based on Structural and Biological Verification of Stachyose as a PPARγ-Modulating Ligand for the Treatment of Non-Alcoholic Fatty Liver Disease. [Abstract]

2025 Sep 22;13(9):e71009. PMID: 40994455
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.
Mol Cell Biochem

Decoding dexmedetomidine's multiple mechanisms in atherosclerosis: effects on lipid metabolism, inflammation, cholesterol efflux, and foam cell formation. [Abstract]

2026 Mar 13. PMID: 41824202
Cell Signal

Serpina3c regulates adipose differentiation via the Wnt/β-catenin-PPARγ pathway. [Abstract]

2022 May:93:110299. PMID: 35263629
Exp Cell Res

Agarotetrol attenuates spinal cord injury by targeting PPARγ to modulate microglial activation. [Abstract]

2026 May 1;458(1):114947. PMID: 41720447
Meat and Muscle Biology

2026.
Front Physiol

Chronic Unpredictable Mild Stress Promotes Atherosclerosis via HMGB1/TLR4-Mediated Downregulation of PPARγ/LXRα/ABCA1 in ApoE-/- Mice. [Abstract]

2019 Mar 1:10:165. PMID: 30881312
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
Am J Physiol Endocrinol Metab

Glycogen synthesis is required for adaptive thermogenesis in beige adipose tissue and affects diet-induced obesity. [Abstract]

2024 May 1;326(5):E696-E708. PMID: 38568151
PPAR Res

Peroxisome Proliferator-Activated Receptor γ Regulates Lipid Metabolism in Sheep Trophoblast Cells through mTOR Pathway-Mediated Autophagy. [Abstract]

2023 Nov 8:2023:6422804. PMID: 38020065
PPAR Res

Activation of PPAR γ Protects Obese Mice from Acute Lung Injury by Inhibiting Endoplasmic Reticulum Stress and Promoting Mitochondrial Biogenesis. [Abstract]

2022 Sep 28:2022:7888937. PMID: 36213491
Adipocyte

Ndufa6 regulates adipogenic differentiation via Scd1. [Abstract]

2021 Dec;10(1):646-657. PMID: 34793269
PPAR Res

Peroxisome Proliferator-Activated Receptor-γ Antagonizes LOX-1-Mediated Endothelial Injury by Transcriptional Activation of miR-590-5p. [Abstract]

2019 Jul 1:2019:2715176. PMID: 31354796
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
Bioorg Med Chem

Design, synthesis, and biological evaluation of novel dual FFA1 and PPARδ agonists possessing phenoxyacetic acid scaffold. [Abstract]

2022 Feb 15:56:116615. PMID: 35051813
J Therm Biol

Differential expression of ADRB1 causes different responses to norepinephrine in adipocytes of Duroc-Landrace-Yorkshire pigs and min pigs. [Abstract]

2024 Jul 2:123:103906. PMID: 38970835
Front Vet Sci

Histological characteristics of hair follicles at different hair cycle and in vitro modeling of hair follicle-associated cells of yak ( Bos grunniens). [Abstract]

2023 Nov 17:10:1277586. PMID: 38046572
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.
Am J Cancer Res

Abrogation of ARF6 promotes RSL3-induced ferroptosis and mitigates gemcitabine resistance in pancreatic cancer cells. [Abstract]

2020 Apr 1;10(4):1182-1193. PMID: 32368394
J Biochem Mol Toxicol

Protective Effect and Mechanism of Rosiglitazone in α-amanitin-induced Hepatotoxicity Via Activation of PPAR-γ/Nrf2 Signaling Pathway. [Abstract]

2026 Feb;40(2):e70701. PMID: 41560421
J Biochem Mol Toxicol

Ferroptosis and Lipid Peroxidation Participate in Valproic Acid-Induced Hepatotoxicity via the Long-chain Acyl-CoA Synthetase 4/Glutathione Peroxidase 4 Pathway. [Abstract]

2025 Oct;39(10):e70484. PMID: 40990894
BMC Gastroenterol

PPARγ activation attenuates neonatal CRD-induced visceral pain sensitization and anxiety in male rats by alleviating oxidative stress. [Abstract]

2025 Jan 20;25(1):22. PMID: 39833676
Fish Physiol Biochem

Promoting adipocyte hyperplasia ameliorates high-carbohydrate diet-induced inflammation, oxidative stress, and metabolic disorders and enhances growth performance and immune function in grass carp (Ctenopharyngodon idellus). [Abstract]

2025 Feb 15;51(2):51. PMID: 39954189
J Cardiovasc Transl Res

TMAO Impairs Mouse Aortic Vasodilation by Inhibiting TRPV4 Channels in Endothelial Cells. [Abstract]

2024 Dec;17(6):1415-1426. PMID: 38980653
Immunol Invest

Absence of TNF Leads to Alternative Activation in Peritoneal Macrophages in Experimental Listeria Monocytogenes Infection. [Abstract]

2022 May;51(4):1005-1022. PMID: 33830841
Biochem Biophys Res Commun

ACSL1 positively regulates adipogenic differentiation. [Abstract]

2024 Nov 26:735:150865. PMID: 39442449
Biochemistry (Mosc)

PTIP Deficiency in B Lymphocytes Reduces Subcutaneous Fat Deposition in Mice. [Abstract]

2021 May;86(5):568-576. PMID: 33993864
Biochem Biophys Res Commun

Curcumin exerts anti-tumor effects on diffuse large B cell lymphoma via regulating PPARγ expression. [Abstract]

2020 Mar 26;524(1):70-76. PMID: 31980182
Endocr J

Rutin promotes white adipose tissue "browning" and brown adipose tissue activation partially through the calmodulin-dependent protein kinase kinase β/AMP-activated protein kinase pathway. [Abstract]

2022 Apr 28;69(4):385-397. PMID: 34719526
Kidney Blood Press Res

Renal NKCC2 Is Dual Regulated by the Synergy of 20-HETE and High-Fat Diet in CYP4F2 Transgenic Mice. [Abstract]

2021;46(5):601-612. PMID: 34320496
Stem Cells Dev

miR-1275 inhibits human omental adipose-derived stem cells differentiation towards the beige phenotype via PRDM16. [Abstract]

2022 Dec;31(23-24):799-809. PMID: 36128801
Orthod Craniofac Res

Compressive Stress and Inflammation Induce Ferroptosis in Periodontal Ligament Cells Through ACSL4 Activation in Orthodontically Induced Inflammatory Root Resorption. [Abstract]

2025 Jun 28. PMID: 40579979
Reprod Domest Anim

PPARγ regulates lipid metabolism and viability of sheep trophoblast cells. [Abstract]

2023 Nov;58(11):1559-1568. PMID: 37712626
Curr Med Sci

Huaier Aqueous Extract Combined with Gefitinib Promotes ACSL4-Dependent Ferroptosis and Overcomes Gefitinib Resistance in Non-Small Cell Lung Cancer. [Abstract]

2026 Feb;46(1):197-211. PMID: 41557244
bioRxiv

Macrophage PIM1 Drives Atherosclerosis by Enhancing Foam Cell Formation Via CD36. [Abstract]

2025 Nov 3:2025.10.31.685966. PMID: 41279778
SSRN

2025 Aug 26.
Res Sq

2025 Aug 11.
SSRN

2025 Mar 18.
SSRN

2025 Feb 5.
Preprints

2024 Aug 23.
hLife

2024 Mar 2.
Research Square Preprint

2024 Feb 7.
Research Square Print

2022 Aug.
Oxid Med Cell Longev

Rosiglitazone Suppresses Renal Crystal Deposition by Ameliorating Tubular Injury Resulted from Oxidative Stress and Inflammatory Response via Promoting the Nrf2/HO-1 Pathway and Shifting Macrophage Polarization. [Abstract]

2021 Oct 14;2021:5527137. PMID: 34691355
Patent

US20180263995A1.
Chinese Pharmacological Bulletin

2017, 33(4): 517-521.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7978 mL

13.9888 mL

27.9775 mL

5 mM

0.5596 mL

2.7978 mL

5.5955 mL

10 mM

0.2798 mL

1.3989 mL

2.7978 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% CMC-Na/saline water

Solubility: 10 mg/mL (27.98 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
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- Français - FR (393 KB)
- Deutsch - DE (393 KB)
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- Español - ES (393 KB)
- Swedish - SV (393 KB)
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- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
Ethanol / DMSO	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

Rosiglitazone

176 Cited Publications

100 mg Angebot einholen

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Rosiglitazone

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

Metabolism/Protease Compound Library

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Publications Citing Use of MedChemExpress (MCE) Rosiglitazone

Alle PPAR Isoform-spezifische Produkte anzeigen

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (176)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Rosiglitazone Related Classifications

Art. -Nr.: HY-17386