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PPARγ Modulator

" in MedChemExpress (MCE) Product Catalog:

43

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3

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14600
    Rosiglitazone maleate
    Maximum Cited Publications
    175 Publications Verification

    BRL 49653C

    PPAR TRP Channel Autophagy Ferroptosis Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone maleate
  • HY-100348

    Androgen Receptor PPAR Apoptosis Cancer
    EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
    EPI-001
  • HY-108022A
    Azemiglitazone potassium
    1 Publications Verification

    MSDC-0602K

    Insulin Receptor PPAR Metabolic Disease
    Azemiglitazone potassium (MSDC-0602K), a PPARγ-sparing thiazolidinedione (Ps-TZD), binds to PPARγ with the IC50 of 18.25 μM . Azemiglitazone potassium modulates the mitochondrial pyruvate carrier (MPC). Azemiglitazone potassium can be used for the research of fatty liver including dysfunctional lipid metabolism, inflammation, and insulin resistance . Azemiglitazone potassium, an insulin sensitizer, improves insulinemia and fatty liver disease in mice, alone and in combination with Liraglutide .
    Azemiglitazone potassium
  • HY-128400

    PARP Metabolic Disease Cancer
    4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity .
    4'-Methoxychalcone
  • HY-101064S3

    PPAR Metabolic Disease
    Fmoc-leucine-d10 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .
    Fmoc-leucine-d10
  • HY-100428

    MCC-555; Isaglitazone

    PPAR Metabolic Disease
    Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus .
    Netoglitazone
  • HY-117103

    INT131

    PPAR Metabolic Disease
    AMG131 (INT131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 is promising for research of type-2 diabetes mellitus .
    AMG131
  • HY-12557

    γ-Glu-Val

    Endogenous Metabolite CaSR Wnt TNF Receptor Interleukin Related PPAR β-catenin Inflammation/Immunology
    γ‑Glutamylvaline (γ-Glu-Val) is a calcium‑sensing receptor (CaSR) agonist. γ‑Glutamylvaline activates CaSR and facilitates its binding to β‑arrestin 2 to modulate inflammatory and metabolic homeostasis signaling. γ‑Glutamylvaline inhibits TNF‑α‑induced IL‑6/MCP‑1 and enhances adiponectin/PPARγ in adipocytes. γ‑Glutamylvaline upregulates Wnt5a, restores β‑catenin phosphorylation, and reduces serine‑phosphorylated IRS‑1 in adipocytes. γ-Glutamylvaline can be used for the research of low-grade chronic inflammation .
    γ-Glutamylvaline
  • HY-101064S2

    N-FMOC-leucine-d3; NPC 15199-d3; NSC 334290-d3

    PPAR Metabolic Disease
    Fmoc-leucine-d3 is the deuterium labeled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .
    Fmoc-leucine-d3
  • HY-108523

    UVI 2112

    RAR/RXR Metabolic Disease
    LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR .
    LG100754
  • HY-101064S1

    Isotope-Labeled Compounds PPAR Metabolic Disease
    Fmoc-leucine- 13C6, 15N is a 15N-labeled and 13C-labled Fmoc-leucine. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity
    Fmoc-leucine-13C6,15N
  • HY-101746

    PPAR Metabolic Disease
    GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus .
    GSK376501A
  • HY-101292

    PPAR Metabolic Disease
    FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes .
    FK614
  • HY-147757

    PPAR Metabolic Disease
    PPARγ/δ modulator 1 (compound 3e) is a potent PPAR modulator. PPARγ/δ modulator 1 is a PPARδ antagonist and a PPARγ partial agonist , with Ki values of 14.4 nM and 5.31 μM, respectively. PPARγ/δ modulator 1 has the EC50 of 7.3 and 12.6 μM for PPARδ corepression and adiponectin production, respectively .
    PPARγ/δ modulator 1
  • HY-160159

    PPAR Metabolic Disease
    Anticancer agent 183 (example 48) is a non-agonistic PPARG modulator. Anticancer agent 183 has a high affinity to PPARG (PPARγ). Anticancer agent 183 inhibits kinase-mediated phosphorylation of PPARG. Anticancer agent 183 can used for research on metabolic diseases to avoid side effects .
    PPARγ modulator-1
  • HY-173622

    PPAR Metabolic Disease Endocrinology
    PPARγ modulator-4 (Compound (I)) is a PPARγ inhibitor (KD: 3.75 μM). PPARγ modulator-4 can inhibit CDK5-mediated phosphorylation of PPARγ at Ser245. PPARγ modulator-4 can be used in insulin resistance research .
    PPARγ modulator-4
  • HY-170874

    PPAR Metabolic Disease
    PPARγ modulator-2 (Compound (R)-2n) is the reversible modulator for PPARγ that inhibits PPARγ ligand-binding domain (LBD) with an IC50 of 41 nM. PPARγ modulator-2 reduces blood glucose, improves the glucose tolerance and insulin tolerance, and exhibits anti-diabetic efficacy in db/db mouse models .
    PPARγ modulator-2
  • HY-176062

    PPAR Metabolic Disease
    PPARγ modulator-3 (Compound 11) is a peroxisome proliferator-activated receptor γ (PPARγ) modulator with a KD value of 186 nM. PPARγ modulator-3 is promising for research of insulin resistance (IR)-related diseases, such as type 2 diabetes mellitus (T2DM) and metabolic syndrome .
    PPARγ modulator-3
  • HY-170581

    PPAR Metabolic Disease
    PPARγ/δ modulator 2 (Compound 3h) is a PPARγ agonist and PPARδ antagonist. The Ki values for PPARγ and PPARδ are 2.8 μM and 43 nM, respectively. PPARγ/δ modulator 2 significantly enhances the production of Adiponectin and promotes adipogenic differentiation of human bone marrow mesenchymal stem cells (hBM-MSCs). PPARγ/δ modulator 2 can be used in the study of metabolic disorders associated with hypoadiponectinemia .
    PPARγ/δ modulator 2
  • HY-151963

    PPAR Glucocorticoid Receptor Metabolic Disease
    PPARγ/GR modulator 1 is an orally active dual agonist of PPARγ and glucocorticoid receptor (GR), with Kis of 3.3 and 33.6 μM, respectively. PPARγ/GR modulator 1 can be used for the research of metabolic diseases, such as diabetes .
    PPARγ/GR modulator 1
  • HY-108572

    PPAR Cardiovascular Disease Metabolic Disease
    S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ .
    S26948
  • HY-163432

    PPAR Metabolic Disease
    YGL-12 is a potent PPARγ modulator with good binding affinity and an IC50 value of 0.85 μM. YGL-12 effectively blocks PPARγ Ser273 phosphorylation and can be used in diabetes research .
    YGL-12
  • HY-B0700

    BRL 49653 sodium

    PPAR TRP Channel Autophagy Metabolic Disease Inflammation/Immunology
    Rosiglitazone sodium is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone sodium is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone sodium
  • HY-14600R

    BRL 49653C (Standard)

    Reference Standards PPAR TRP Channel Autophagy Ferroptosis Metabolic Disease Inflammation/Immunology Cancer
    Rosiglitazone (maleate) (Standard) is the analytical standard of Rosiglitazone (maleate). This product is intended for research and analytical applications. Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).
    Rosiglitazone maleate (Standard)
  • HY-118397

    PPAR Others
    RB394 is a potent dual sEH/PPARγ modulator isoform that promotes adipocyte browning and exhibits cardioprotective activity, and can be used to suppress metabolic syndrome.
    RB394
  • HY-126969

    PPAR Metabolic Disease
    C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
    C333H
  • HY-147705

    PPAR Metabolic Disease
    PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC50 of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC50 of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects .
    PPARγ phosphorylation inhibitor 1
  • HY-W109107

    PPAR TGF-beta/Smad Interleukin Related Inflammation/Immunology
    GED 0507-34-Levo is an orally active PPARγ modulator. GED 0507-34-Levo downregulates the expression of TGF-β, Smad3, IL-13, and CTGF in the colon. GED 0507-34-Levo improves DSS-induced chronic colitis and fibrosis .
    GED 0507-34-Levo
  • HY-128400R

    PARP Reference Standards Metabolic Disease Cancer
    4'-Methoxychalcone (Standard) is the analytical standard of 4'-Methoxychalcone. This product is intended for research and analytical applications. 4'-Methoxychalcone regulates adipocyte differentiation through PPARγ activation. 4'-Methoxychalcone modulates the expression and secretion of various adipokines in adipose tissue that are involved in insulin sensitivity .
    4'-Methoxychalcone (Standard)
  • HY-100428R

    MCC-555 (Standard); Isaglitazone (Standard)

    Reference Standards PPAR Metabolic Disease
    Netoglitazone (Standard) is the analytical standard of Netoglitazone (HY-100428). This product is intended for research and analytical applications. Netoglitazone (MCC-555) is an orally active PPARγ ligand with an EC50 of 8 μM. Netoglitazone mediates cell type-specific functional regulation, and modulates the transcriptional activity of PPARγ as a full agonist, partial agonist or antagonist. Netoglitazone induces adipogenesis, inhibits osteoblastogenesis, alters the weight of extramedullary fat depots and enhances insulin sensitivity. Netoglitazone reduces blood glucose levels. Netoglitazone can be used in research related to type 2 diabetes and non-insulin-dependent diabetes mellitus .
    Netoglitazone (Standard)
  • HY-172883

    FABP PPAR Metabolic Disease Inflammation/Immunology
    ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC50 s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
    ABP/PPAR modulator 1
  • HY-172883A

    FABP PPAR Metabolic Disease Inflammation/Immunology
    (E/Z)-ABP/PPAR modulator 1 is a mixture of the E and Z isomers of ABP/PPAR modulator 1 (HY-172883). ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC50 s of 9.19  μM, 2.20  μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model .
    (E/Z)-ABP/PPAR modulator 1
  • HY-117103A

    INT131 benzenesulfonate

    PPAR Metabolic Disease
    AMG131 (INT131) (benzenesulfonate) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 (benzenesulfonate) binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 (benzenesulfonate) is promising for research of type-2 diabetes mellitus .
    AMG131 benzenesulfonate
  • HY-179015

    17β-HSD PPAR Metabolic Disease Inflammation/Immunology
    HSD17B13/PPAR modulator-1 (Compound 17) is a HSD17B13/PPAR multitarget modulator. HSD17B13/PPAR modulator-1 is an inhibitor of HSD17B13, with its IC50 value being 0.91 μM. HSD17B13/PPAR modulator-1 is a PPAR agonist, with the EC50 values for PPARα, PPARδ, and PPARγ being 1.55, 0.12, and 0.01 μM respectively. HSD17B13/PPAR modulator-1 can significantly improve liver function, regulate lipid metabolism, alleviate fibrosis, and exert antioxidant and anti-inflammatory effects in the model of metabolic dysfunction-related steatohepatitis (MASH). HSD17B13/PPAR modulator-1 can be used for the study of MASH .
    HSD17B13/PPAR modulator-1
  • HY-161926

    PPAR Metabolic Disease
    YGT-31 is a modulator for PPARγ with an IC50 of 1.72 μM, and a Ki of 0.62 μM. YGT-31 reduces blood glucose levels and improves insulin resistance in db/db mice type 2 diabetes models, through inhibition of CDK5-mediated PPARγ-Ser273 phosphorylation. YGT-31 exhibits anti-hepatic steatosis effect in mice non-alcoholic fatty liver disease (NAFLD) model .
    YGT-31
  • HY-100348R

    Reference Standards Androgen Receptor PPAR Apoptosis Cancer
    EPI-001 (Standard) is the analytical standard of EPI-001. This product is intended for research and analytical applications. EPI-001, a selective inhibitor of Androgen Receptor (AR), targets transactivation unit 5 (Tau-5) of the AR. EPI-001 can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of ~6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 is active against castration-resistant prostate cancer .
    EPI-001 (Standard)
  • HY-116115

    17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA

    NF-κB PPAR Inflammation/Immunology
    17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid (17-Oxo-DPA; 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-DPA) is an electrophilic oxo-derivative (EFOX) of the docosahexaenoic acid (DHA) (HY-B2167). 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid is generated during inflammation by COX-2-catalyzed mechanism in activated macrophages. 17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid acts as an agonist for PPARγ and a modulator for NF-κB signaling pathway, inhibits the production of pro-inflammatory cytokines and nitric oxide, and exhibits anti-inflammatory efficacy .
    17-Oxo-7(Z),10(Z),13(Z),15(E),19(Z)-docosapentaenoic acid
  • HY-101292R

    PPAR Reference Standards Metabolic Disease
    FK614 (Standard) is the analytical standard of FK614 (HY-101292). This product is intended for research and analytical applications. FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes .
    FK614 (Standard)
  • HY-101064R

    N-FMOC-leucine (Standard); NPC 15199 (Standard); NSC 334290 (Standard)

    PPAR Reference Standards Metabolic Disease
    Fmoc-leucine (Standard) is the analytical standard of Fmoc-leucine (HY-101064). This product is intended for research and analytical applications. Fmoc-leucine is a selective PPARγ modulator. Fmoc-leucine activates PPARγ with a lower potency but a similar maximal efficacy than rosiglitazone. Fmoc-leucine improves insulin sensitivity in normal, diet-induced glucose-intolerant, and in diabetic db/db mice. Fmoc-leucine has a lower adipogenic activity .
    Fmoc-leucine (Standard)
  • HY-180398

    PPAR PGC-1α Metabolic Disease
    PA-082 is a selective PPAR-γ modulator that functions as a partial agonist. PA-082 causes partial recruitment of SRC1, TIF2, SRC3 and full recruitment of PGC1-α to PPAR-γ ligand-binding domain. PA-082 prevents triglyceride accumulation during de novo adipogenesis and antagonizes Rosiglitazone (HY-17386)-induced lipid accumulation. PA-082 potentiates insulin-stimulated glucose uptake in adipocytes and protects against TNFα-induced insulin resistance. PA-082 can be used for the research of type 2 diabetes .
    PA-082
  • HY-108523R

    UVI 2112 (Standard)

    Reference Standards RAR/RXR Metabolic Disease
    LG100754 (Standard) is the analytical standard of LG100754 (HY-108523). This product is intended for research and analytical applications. LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXR homodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR .
    LG100754 (Standard)
  • HY-122222

    PPAR Others
    MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC50 being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC50 values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .
    MRL20
  • HY-N17617

    Phosphodiesterase (PDE) Apoptosis NO Synthase Caspase PPAR Bcl-2 Family PARP Metabolic Disease Inflammation/Immunology Cancer
    S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis .
    S-Petasin

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