PPAR

Cat. No.

A12413

CAS No.

436159-64-7

GW6471

GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.

Cat. No.

A11588

CAS No.

313516-66-4

T0070907

T0070907 was identified as a potent and selective PPARgamma antagonist. With an apparent binding affinity (concentration at 50% inhibition of [(3)H]rosiglitazone binding or IC(50)) of 1 nm, T0070907 covalently modifies PPARgamma on cysteine 313 in helix 3 of human PPARgamma2.

Cat. No.

A11984

CAS No.

22978-25-2

GW 9662

GW 9662 is a selective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively).

Cat. No.

A12391

CAS No.

188591-46-0

GSK-3787

GSK-3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6).

Cat. No.

A12392

CAS No.

1014691-61-2

GSK 0660

GSK 0660 is a selective PPARβ antagonist (IC50 values are 0.155, > 10 and ??? 10 μM at PPARβ, PPARα and PPARγ respectively).

Cat. No.

A18771

CAS No.

1454925-59-7

NXT629

NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively.

Cat. No.

A19926

CAS No.

120128-20-3

RG-12525

Synonyms: NID 525

RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.

Cat. No.

A21934

CAS No.

880635-03-0

GW 6471

GW 6471 is a potent PPARα antagonist.

Cat. No.

A39914

CAS No.

1338259-05-4

SR1664

SR1664 is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ). It effectively binds to PPARγ and inhibits Cdk5-mediated phosphorylation of the receptor, demonstrating an IC50 value of 80 nM and a Ki of 28.67 nM. This compound has valuable applications in research focused on metabolic regulation and the development of therapeutic strategies for conditions such as obesity and diabetes.

Cat. No.

A39926

CAS No.

76541-72-5

Mifobate

Synonyms: SR-202

Mifobate is a potent antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), selectively inhibiting thiazolidinedione (TZD)-induced transcriptional activity with an IC50 of 140 μM. This compound does not affect the basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate demonstrates significant antiobesity and antidiabetic effects, making it valuable for research applications aimed at exploring metabolic disorders and therapeutic interventions for related conditions.

Cat. No.

A39951

CAS No.

36099-95-3

H-Trp-Glu-OH

Synonyms: G3335

H-Trp-Glu-OH is a selective and reversible antagonist of peroxisome proliferator-activated receptor gamma (PPARγ), with a dissociation constant (Kd) of approximately 8 µM. This compound has demonstrated cell permeability and presents potential as a lead compound in diabetes research. Its role in modulating PPARγ activity makes it an important tool for studying metabolic disorders and associated therapeutic pathways.

Cat. No.

A39968

CAS No.

1616372-41-8

Amezalpat

Synonyms: TPST-1120

Amezalpat is a selective antagonist of PPARα, exhibiting an IC50 value of 58 nM. This compound demonstrates notable antineoplastic activity, making it a valuable tool for research in cancer biology and therapeutic applications targeting metabolic regulation and lipid homeostasis. Its use in scientific studies may help elucidate the role of PPARα in tumor progression and treatment resistance.

Cat. No.

A39984

CAS No.

1820602-13-8

SR 11023

SR 11023 is a potent orally active antagonist of PPARγ, exhibiting an IC50 value of 109 nM. This compound is significant in the study of metabolic disorders, particularly in diabetes research, where PPARγ modulation can impact insulin sensitivity and adipocyte differentiation. Researchers can utilize SR 11023 to investigate the therapeutic potential of targeting PPARγ in various metabolic pathways.

Cat. No.

A40018

CAS No.

1060968-92-4

E17241

E17241 is an inducer of ATP-binding cassette transporter A1 (ABCA1) that significantly enhances ABCA1 protein levels in RAW 264.7 macrophages. It also acts as an agonist for peroxisome proliferator-activated receptors (PPARs), contributing to metabolic regulation. Notably, E17241 has demonstrated the capability to reduce plasma glucose levels and body weight in KKAy diabetic mice subjected to a high-fat and high-glucose diet, making it a valuable reagent for research on lipid metabolism and diabetes management.

Cat. No.

A40048

CAS No.

1258011-97-0

OLHHA

OLHHA is a dual CB1 receptor antagonist and PPARα agonist. This compound demonstrates notable activity in inhibiting alcohol intake with an EC50 value of 0.2 mg/kg. Additionally, OLHHA effectively reduces hepatic lipid accumulation and circulating triglyceride levels, exhibiting anti-steatotic properties. Its mechanism and effects make it a valuable tool for research into non-alcoholic fatty liver disease (NAFLD).

Cat. No.

A40071

CAS No.

1680204-90-3

CC618

CC618 is a selective antagonist of the peroxisome proliferator-activated receptor beta/delta (PPARβ/δ). This compound exhibits its antagonistic effects by covalently binding to PPARβ/δ receptors, modulating their activity. As a result, CC618 is valuable for exploring the roles of PPARβ/δ in various biological processes and disease states, making it a useful tool in metabolic research and studies related to inflammation and cancer.

Cat. No.

A40125

CAS No.

149437-51-4

LTD4 antagonist 3

Synonyms: FK011 hydrochloride

LTD4 antagonist 3 (FK011 hydrochloride) is a selective leukotriene D4 (LTD4) antagonist that also exhibits agonistic activity for peroxisome proliferator-activated receptor gamma (PPAR-γ). This compound demonstrates enhanced PPAR-γ activation with a fold-increase of 1.50 at 1 μM and 2.35 at 10 μM. LTD4 antagonist 3 is valuable for research in the development of non-steroidal anti-inflammatory drugs (NSAIDs) and related therapeutic applications targeting inflammatory pathways.

Cat. No.

A40168

CAS No.

1356497-92-1

PT-S58

PT-S58 is a PPARβ/δ antagonist exhibiting potent inhibitory activity with an IC50 value of 98 nM. This compound effectively blocks agonist-induced transcriptional activity of PPARβ/δ in vitro, making it a valuable tool for studying the functional roles of this receptor in various biological processes. Its application extends to research on metabolic disorders, inflammation, and cancer biology.