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.

A11900

CAS No.

6197-30-4

Octocrylene

Octocrylene is an organic ultraviolet (UV) filter primarily known for absorbing UVB radiation and shorter UVA wavelengths. This compound acts as a partial agonist of PPARγ, influencing the transcription profiles of lipid metabolism enzymes. Additionally, Octocrylene exhibits cytotoxic and genotoxic effects on human skin fibroblasts and has been shown to mediate the biosynthesis of estrogens, such as estriol, in zebrafish larvae while impacting antioxidant pathways, including glutathione transferase and peroxisomes. Its applications include studies in photoprotection, environmental toxicology, and endocrine disruption research.

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.

A15013

CAS No.

199113-98-9

Balaglitazone

Synonyms: DRF-2593; NN-2344

Balaglitazone is a novel partial agonist of PPAR-gamma (γ).

Cat. No.

A15695

CAS No.

57396-78-8

Oroxin A

Oroxin A is a partial agonist of the peroxisome proliferator-activated receptor gamma (PPARγ). It enhances PPARγ transcriptional activity through binding to the PPARγ ligand-binding domain. Additionally, Oroxin A demonstrates inhibitory effects on α-glucosidase and possesses antioxidant properties. Its anti-breast cancer potential is attributed to the induction of endoplasmic reticulum stress-mediated cellular senescence, making it a valuable tool for research in metabolic and cancer biology.

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.

A21135

CAS No.

24136-23-0

Arhalofenate

Synonyms: MBX 102; JNJ 39659100

Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

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.

A39991

CAS No.

870554-67-9

GQ-16

GQ-16 is an orally active partial agonist of PPARγ, exhibiting an IC50 of 1.84 μM and a Ki of 160 nM against human PPARγ. This compound effectively inhibits Cdk5-mediated Ser-273 phosphorylation, enhancing insulin sensitivity and glucose tolerance in obese and diabetic mouse models. Additionally, GQ-16 demonstrates cytotoxic effects against various tumor cell lines, making it a valuable reagent for research on obesity, diabetes, and cancer.

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.

A40052

CAS No.

23953-39-1

MBX-102 acid

MBX-102 acid is a selective partial agonist of PPAR-γ (Peroxisome Proliferator-Activated Receptor Gamma). This compound exhibits strong binding to plasma proteins, primarily serum albumin, which may influence its pharmacokinetics. MBX-102 acid is primarily utilized in research related to type 2 diabetes, aiding in the exploration of its role in glucose metabolism and insulin sensitivity.

Cat. No.

A40063

CAS No.

52936-64-8

Caulophyllogenin

Caulophyllogenin is a triterpene saponin that acts as a partial agonist of PPARγ, exhibiting an EC50 of 12.6 μM. This compound plays a significant role in the modulation of glucose metabolism and adipogenesis, making it relevant for research on type-2 diabetes, obesity, metabolic syndrome, and inflammation. Its distinct biological activity allows for further exploration in the development of therapeutic strategies targeting metabolic disorders.

Cat. No.

A40069

CAS No.

18446-70-3

Neoambrosin

Neoambrosin is a sesquiterpene lactone that acts as a partial agonist of the PPARγ and TRPA1 receptors. This compound demonstrates potential biological activity related to hypoglycemia, analgesia, anti-inflammatory responses, and anticancer effects. Neoambrosin is suitable for research applications aimed at exploring metabolic disorders and pain management, as well as studying its role in inflammation and cancer therapeutics.

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.

A40079

CAS No.

1067214-81-6

GSK-7227

GSK-7227 is a partial agonist of the peroxisome proliferator-activated receptor delta (PPARδ). It effectively regulates the expression of target genes associated with lipid metabolism, specifically CPT1a and PDK4, in skeletal muscle cells. This compound holds potential for studies focused on metabolic disorders and mitochondrial function modulation.

Cat. No.

A40085

CAS No.

1168138-37-1

GSK 1997132B

GSK 1997132B is a benzimidazole-derived partial agonist of PPARγ, notable for its ability to cross the blood-brain barrier with a pEC50 value of 8.0. This compound selectively activates PPARγ while exhibiting minimal activity on PPARα and PPARδ, addressing issues related to high blood clearance rates seen in earlier agents. GSK 1997132B is particularly relevant for research into Alzheimer's disease, providing a potential pathway for exploring therapeutic strategies that mitigate associated side effects such as weight gain and edema.