PPAR

PPAR

Peroxisome proliferator-activated receptors

PPAR

Related Products

PPARs (Peroxisome proliferator-activated receptors) are ligand-activated transcription factors of nuclear hormone receptor superfamily comprising of the following three subtypes: PPARα, PPARγ, and PPARβ/δ. PPARs play essential roles in the regulation of cellular differentiation, development, and metabolism (carbohydrate, lipid, protein), and tumorigenesis of higher organisms. All PPARs heterodimerize with the retinoid X receptor (RXR) and bind to specific regions on the DNA of target genes. Activation of PPAR-α reduces triglyceride level and is involved in regulation of energy homeostasis. Activation of PPAR-γ enhances glucose metabolism, whereas activation of PPAR-β/δ enhances fatty acids metabolism.

PPAR Isoform Specific Products:

PPAR Isoform Comparison

PPAR Related Products (515)
Recombinant Proteins (9)
Antibodies (4)
PPAR Isoform Comparison

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By Effects:	Controls (4) Inhibitors (69) Ligand (1) Agonists (265) Antagonists (23) Activators (91) Modulators (25) Inducers (5)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-160003

PPARγ agonist 9	Agonist
PPARγ agonist 9 is an agonist of PPARγ. PPARγ agonist 9 is the analogue of lysophosphatidic acid with an EC₅₀ more than 10 μM for LPA₃ receptor.

HY-17386S1

Rosiglitazone-d₄	Agonist
Rosiglitazone-d₄ is deuterated labeled Rosiglitazone (HY-17386). Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

HY-B0258S1

Gemfibrozil-d₆-1	Activator
Gemfibrozil-d6-1 (CI-719-d6-1) is the deuterium labeled Gemfibrozil (HY-B0258). Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with K_i values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.

HY-120255A

17(S)-HDHA	Activator
17(S)-HDHA is a pro-resolving mediator (SPM). 17(S)-HDHA slightly activats PPARγ, PPARα and PPARδ.

HY-N2118R

Bilobetin (Standard)	Activator
Bilobetin (Standard) is the analytical standard of Bilobetin. This product is intended for research and analytical applications. Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.

HY-122083

T2384	Activator
T2384 is a peroxisome proliferator-activated receptor γ (PPARγ) ligand. T2384 also is an orally active antidiabetic agent. T2384 reduces the fasting plasma glucose levels and plasma insulin levels.

HY-B0760S1

Fenofibric acid-¹³C₈	Agonist
Fenofibric acid-¹³C₈ (FNF acid-¹³C₈) is ¹³C labeled Fenofibric acid. Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC₅₀s of 22.4 μM, 1.47 μM, and 1.06 μM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC₅₀ of 48 nM.

HY-15027S3

5-Aminosalicylic acid-d₃ disodium	Agonist
5-Aminosalicylic acid-d₃ disodium is deuterated labeled 5-Aminosalicylic Acid (HY-15027). 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

HY-50935R

Troglitazone (Standard)	Agonist
Troglitazone (Standard) is the analytical standard of Troglitazone. This product is intended for research and analytical applications. Troglitazone is an orally active PPARγ agonist, with EC₅₀s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.

HY-N10612

Petasin	Inhibitor
Petasin inhibits adipogenesis in cell 3T3-F442A with an IC₅₀ of 0.95 μM. Petasin inhibits the expression of lipid synthesis factors ACC1, FAS and SCD1 by inhibiting transcription factors PPARγ and C/EBPα, as well as targeting TRPA1 and TRPV1 channels . Petasin inhibits mitochondrial complex I, thereby inhibiting tumor growth and metastasis. Petasin activates AMPK signaling pathway, participating in regulation of glucose and lipid metabolism. Petasin is orally active.

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].

HY-118788

N-Desmethyl rosiglitazone	Agonist
N-Desmethyl rosiglitazone (SB 237216) is a metabolite of Rosiglitazone (HY-17386), generated through demethylation by the cytochrome P450 enzyme system in liver microsomes. It retains partial PPARγ agonist activity and supports studies on the metabolism and pharmacokinetics of Rosiglitazone (HY-17386).

HY-10838R

GW 501516 (Standard)	Agonist
GW 501516 (Standard) is the analytical standard of GW 501516. This product is intended for research and analytical applications. GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM.

HY-138007

SR-1903	Antagonist
SR-1903 is an inverse agonist of RORγ and PPARγ (IC₅₀ of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.

HY-W009066

2-Ethylhexyl diphenyl phosphate	Agonist
2-Ethylhexyl diphenyl phosphate is an organophosphate flame retardants (OPFRs) and a PPARG agonist (EC₂₀: 2.04 µM). 2-Ethylhexyl diphenyl phosphate also inhibits ERRγ transcriptional activity (IC₅₀: 1.3 µM). 2-Ethylhexyl diphenyl phosphate upregulates 3β-HSD1, human chorionic gonadotropin (hCG) and progesterone secretion. 2-Ethylhexyl diphenyl phosphate can be used in studies of female reproduction and fetal development.

HY-113655

AD-5075
AD-5075 is an orally active insulin sensitizer. AD-5075 mediates its antidiabetic activity by binding to PPARγ and thereby generating an active conformation of the receptor.

HY-17386R

Rosiglitazone (Standard)	Agonist
Rosiglitazone (Standard) is the analytical standard of Rosiglitazone. This product is intended for research and analytical applications. Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

HY-167950

PPARα/γ agonist 5	Agonist
PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC₅₀ of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy.

HY-16737A

(E/Z)-Elafibranor	Agonist
(E/Z)-Elafibranor ((E/Z)-GFT505) is a PPARα/δ agonist with EC₅₀s of 45 and 175 nM, respectively.

HY-128932R

Cefminox (sodium) (Standard)	Agonist
Cefminox (sodium) (Standard) is the analytical standard of Cefminox (sodium). This product is intended for research and analytical applications. Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits a broad spectrum of antibacterial activity. Cefminox sodium (MT-141) also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ, upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium (MT-141) also prevents pulmonary arterial hypertension.

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