PPAR Modulator

BAY-9683 is an orally active covalent PPARG inverse agonist. BAY-9683 can be used in the study of diseases with overactive PPARG, such as luminal bladder cancer.

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.

SR2595 is an inverse agonist of PPARγ with an IC₅₀ of 30 nM.

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.

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.

Perfluoroenanthic acid-¹³C₄ (Perfluoroheptanoic acid-¹³C₄) is the ¹³C-labeled Perfluoroenanthic acid (HY-21197). Perfluoroenanthic acid (Perfluoroheptanoic acid) is a kind of perfluoroalkyl carboxylic acid organic pollutant. Perfluoroenanthic acid has environmental persistence and bioaccumulation, and exposure can occur via oral, dermal and other routes. Perfluoroenanthic acid exhibits reproductive toxicity, neurotoxicity, hepatotoxicity, immunotoxicity and endocrine-disrupting effects. Perfluoroenanthic acid exerts definite adverse effects on development, spermatogenesis, neuronal activity and liver tissue.

CRX000227 is a PPAR modulator. CRX000227 can be used for research of metabolic or cell proliferative disorders.

(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.

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.

PPARγ modulator-3 (Compound 11) is a peroxisome proliferator-activated receptor γ (PPARγ) modulator with a K_D 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.

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.

YGT-31 is a modulator for PPARγ with an IC₅₀ of 1.72 μM, and a K_i 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.

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.

GQ-16 (Standard) is the analytical standard of GQ-16 (HY-111254). This product is intended for research and analytical applications. GQ-16 is an orally active PPARγ partial agonist with an IC₅₀ of 1.84 μM and a K_i of 160 nM against human PPARγ. GQ-16 inhibits Cdk5-mediated Ser-273 phosphorylation. GQ-16 improves insulin sensitivity and glucose tolerance in obese and diabetic mice. GQ-16 also exhibits certain cytotoxicity against tumor cells. GQ-16 can be used in research related to obesity, diabetes and cancer.

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.

Azemiglitazone (Standard) is the analytical standard of Azemiglitazone (HY-108022). This product is intended for research and analytical applications. Azemiglitazone (MSDC-0602) is an orally active thiazolidinedione (TZD) -like molecule, which binds to PPARγ with low binding and activating affinity. Azemiglitazone inhibits mitochondrial pyruvate carrier (MPC), which inhibits Alzheimer’s disease and diminishes nonalcoholic steatohepatitis (NASH) caused liver injury.

Perfluoropentanoic acid (Standard) (PFPeA (Standard)) is the analytical standard of Perfluoropentanoic acid (HY-21193). This product is intended for research and analytical applications. Perfluoropentanoic acid (PFPeA), a short-chain perfluorinated compound, serves as an important indicator of perfluorinated compound pollution in ecosystems. Perfluoropentanoic acid exhibits certain toxicity to mice.

Aminophylline (Standard) is the analytical standard of Aminophylline (HY-B0140). This product is intended for research and analytical applications. Aminophylline is a competitive phosphodiesterase 3/4 (PDE3/4) inhibitor. Aminophylline also acts as an adenosine receptor antagonist. Aminophylline elevates intracellular cAMP levels via competitive inhibition of PDE3 and PDE4, antagonizes adenosine A1 receptor (ADORA1), regulates intracellular calcium signaling and synaptic vesicle cycling, upregulates the PPAR signaling pathway, and downregulates glutamatergic synaptic pathways simultaneously. Aminophylline can be used in research related to major depressive disorder, epilepsy, asthma, and chronic obstructive pulmonary disease (COPD).

Fmoc-Ala-OH-¹³C3 is a ¹³C-labeled Fmoc-Ala-OH (HY-W009204). Fmoc-Ala-OH is an alanine derivative.

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.