PPAR Modulator

PPAR Modulators (21):

Cat. No.	Product Name	Effect	Purity

HY-108022

Azemiglitazone	Modulator
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.

HY-100348

EPI-001	Modulator	98.87%
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.

HY-101064

Fmoc-leucine	Modulator	99.91%
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.

HY-134377

Bocidelpar	Modulator	98.08%
Bocidelpar is a modulator of peroxisome proliferator-activated receptor delta (PPAR-δ). Bocidelpar improves mitochondrial biogenesis and function in Duchenne Muscular Dystrophy (DMD) muscle cells (extracted from patent WO2017062468A1, compound 2b).

HY-108022A

Azemiglitazone potassium	Modulator	99.53%
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.

HY-111254

GQ-16	Modulator	98.88%
GQ-16 is a moderate affinity ligand for the ligand-binding domain (LBD) of PPARγ, exhibiting a K_i of 160 nM. GQ-16 is an effective inhibitor of Cdk5-mediated phosphorylation of PPARγ. GQ-16 is a partial agonist of PPARγ with reduced adipogenic actions. GQ-16 promotes insulin Sensitization without weight gain.

HY-114739

MA-0204	Modulator	99.31%
MA-0204 is a potent, highly selective and orally available peroxisome proliferator activated receptor δ (PPARδ) modulator with EC₅₀s of 0.4 nM, 7.9 nM and 10 nM for human, mouse and rat PPARδ, respectively. Potential treatment for Duchene Muscular Dystrophy (DMD).

HY-163432

YGL-12	Modulator
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.

HY-147757

PPARγ/δ modulator 1	Modulator
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 K_i 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.

HY-101064S1

Fmoc-leucine-¹³C₆,¹⁵N	Modulator
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

HY-160188

BAY-9683	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.

HY-116521

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

HY-160159

PPARγ modulator-1	Modulator
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.

HY-153759

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

HY-W009204S5

Fmoc-Ala-OH-¹³C₃	Modulator
Fmoc-Ala-OH-¹³C₃ is a ¹³C-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-ind

HY-100348R

EPI-001 (Standard)	Modulator
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.

HY-161926

YGT-31	Modulator
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.

HY-101064S3

Fmoc-leucine-d₁₀	Modulator	98.90%
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[1].

HY-117103A

AMG131 benzenesulfonate	Modulator
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.

HY-101064S2

Fmoc-leucine-d₃	Modulator	98.50%
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[1].

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