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PPAR and RXR Regulators

PPAR Signaling Pathway
Similar to other nuclear hormone receptors, peroxisome proliferator-activated receptors (PPARs) act as ligand-activated transcription factors. When bound to its fatty acid ligand, PPARα forms a heterodimeric complex with the retinoid X receptor (RXR) to regulate transcription. PPARγ is activated by prostaglandins and leukotrienes and regulates the gene expression of proteins involved in the storage of fatty acids. PPARβ is weakly activated by fatty acids, prostaglandins, and leukotrienes. Its physiological ligand has not been identified.
References:
Fajas, L., et al., Peroxisome proliferator-activated receptor-gamma: from adipogenesis to carcinogenesis. J. Mol. Endocrinol., 27, 1-9 (2001).
Qi, C., et al., Peroxisome proliferator-activated receptors, coactivators, and downstream targets. Cell. Biochem. Biophys., 32, 187-204 (2000).

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Description	Biochem/physiol Actions	Product #
AC-41848 hydrate ≥98% (HPLC), solid	AC-41848 is a potent, cell permeable, subtype selective retinoic acid receptor RARγ agonist. AC-41848 has high selectivity (92%) for RARγ. EC₅₀= 5.9 μM.	A7980
AC-55649 ≥98% (HPLC), solid	AC-55649 is a subtype selective RAR (RARβ2) agonist. AC-55649 is a potent, orally available isoform selective Retinoic Acid Receptor β2. AC-55649 has high selectivity, 99% for RARβ2 and 31% for RARβ1. When compared to the gold standard AM-580 (Cat. No A8843), both isoform receptors were 100%. AC-55649 has a potent EC₅₀ of 6.9 μM compared to an EC₅₀ of 7.7 μM for AM-580.	A9480
AC-93253 iodide ≥98% (HPLC), solid	AC-93253 is a potent, cell permeable, subtype selective RAR (RARα) agonist. EC₅₀ = 6.3 μM. AC-93253 has high selectivity; 89% for RARα vs 67% for RARβ1, 35% for RARβ2, and 11% for RARγ.	A9605
AM580 98% (TLC)		A8843
Azelaoyl PAF 10 mg/mL in ethanol	Potent PPARγ agonist.	A6850
Bezafibrate ≥98%, solid	The peroxisome proliferator-activated receptor (PPAR) is a member of the steroid nuclear receptor superfamily. Bezafibrate is a peroxisome proliferator-activated receptor agonist for PPARα, PPARδ, and PPARγ. Lipoprotein lipase (LPL) activator. PPARgamma agonists, including Bezafibrate, have beneficial effects in the suppression of the inflammatory response during RSV infection and therefore might have clinical efficacy in the course of severe RSV-infection.	B7273
Bisphenol A diglycidyl ether	PPARγ inhibitor that blocks rosiglitazone- and insulin-induced adipogenesis.	D3415
2-Bromohexadecanoic acid ~97%	PPARδ agonist	238422
CD437 ≥98% (HPLC), solid	CD437 hemihydrate is a retinoic acid receptor, γ-selective retinoid; potent inducer of apoptosis in human lung, cervical, and breast cancer cells.	C5865
Ciglitizone ≥99% (TLC)	Selective peroxisome proliferator-activated receptor-γ (PPARγ) agonist (EC₅₀ = 3 μM) and antihyperglycemic agent displaying activity in genetically obese C57 B1/6 ob/ob mice.	C3974
Ciprofibrate	Peroxisome proliferator-activated receptor α (PPARα) agonist	C0330
DRF 2519 ≥98% (HPLC), solid	DRF-2519 is a dual PPARα/γ activator. DRF-2519 has better reduction of plasma insulin, triglyceride, and free fatty acid levels than those treated with rosiglitazone.	D6567
GW0742 ≥98% (HPLC), solid	GW0742 is a highly selective PPARδ agonist. EC₅₀= 1 nM vs 1 and 2 mM for PPARα and PPARγ, respectively.	G3295
GW1929 hydrate >98% (HPLC), solid	GW1929 is a high affinity agonist of PPAR-γ.	G5668
GW3965 hydrochloride ≥98% (HPLC), solid	GW3965 is a liver X receptor full agonist on hLXRα and hLXRβ. GW3965 has an EC₅₀= 125 nM in a cell-free ligand-sensing assay of LXRα and profiles as a full agonist on hLXRα and hLXRβ in cell-based assays with EC₅₀ = 190 nM and 30 nM, respectively. It is orally active in mice. When screened against a panel of nuclear receptors, it cross-reacted with only the pregnane X receptor (PXR). The literature agonist, T0901317 (Tularik), had an EC₅₀= 60 nM and 85 nM in the cell-free and cell-based assays, respectively.	G6295
GW4716 ≥98% (HPLC), solid	GW4716 is an estrogen-related receptor γ (ERRγ) agonist. The ERRs generally are considered to be constitutively active receptors that interact with coactivator proteins in the absence of exogenous ligands. IC₅₀ value of 300-500 nM in transient transfection assays.	G5920
GW6471 ≥98% (HPLC), solid	GW6471 is a PPARα antagonist, which completely inhibits GW409544-induced activation of PPARα with an IC₅₀ = 0.24 μM. GW6471 induces a PPARα conformation that interacts efficiently with co-repressors.	G5045
GW7647 ≥98% (HPLC)	Potent human PPARα agonist. Use to study the biology of PPARα receptor in human cells.	G6793
GW9662 >98% (HPLC), solid	GW9662 is an irreversible PPARγ antagonist. GW9662 inhibits connective tissue growth factor and activation of CD36 by IL-4.	M6191
13(S)-Hydroxyoctadeca-9Z,11E-dienoic acid ~100 μg/mL in ethanol, ~98%	Expression of 15-lipoxygenase-1 (15-LOX-1) and its main product, 13(S)-HODE, are decreased in human colorectal and esophageal cancers. Certain non-steroidal anti-inflammatory drugs (NSAIDs) can induce apoptosis in human colon cancer cells by increased expression of 15-LOX-1, which down-regulates PPAR-delta through 13-HODE. PPARγ agonist	H9146
L-165,041 ≥98% (HPLC), solid	PPARβ (PPARδ) selective agonist.	L2167
N-(3-Oxooctanoyl)-L-homoserine lactone ≥97% (HPLC), white powder	Stimulates tra gene expression. Autoinducer and potent antagonist.	O1764
Retinoic acid ≥98% (HPLC), powder	all−trans−Retinoic acid (ATRA) is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR). The bound RAR and RXR act as transcription factors that regulate the growth and differentiation of both normal and malignant cells. Cytochromes P450 (CYPs) catalyze the 4-hydroxylation of ATRA. Retinoic acid primes embryonic stem cells to become neurons.	R2625
9-cis-Retinoic acid ~98% (HPLC)	Ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR) that act as transcription factors to regulate the growth and differentiation of normal and malignant cells.	R4643
13-cis-Retinoic acid ≥98% (HPLC)	13-cis-Retinoic acid (RA) has anti-inflammatory and anti-tumor action. The action of RA is mediated through RAR-β and RAR-α receptors. RA attenuates iNOS expression and activity in cytokine-stimulated murine mesangial cells. It induces mitochondrial membrane permeability transition, observed as swelling and as a decrease in membrane potential, and stimulates the release of cytochrome c implicating mechanisms through the apoptosis pathway. These activities are reversed by EGTA and cyclosporin A. RA also increases MMP-1 protein expression partially via increased transcription.	R3255
Retinoic acid p-hydroxyanilide ≥95%	Vitamin A acid analogue with antiproliferative activity in cultured human breast cancer cells; induces apoptosis in malignant hemopoietic cell lines.	H7779
SR-202 ≥98% (HPLC), crystalline	Selective PPARγ antagonist. Feeding mice with a high-fat diet induced insulin resistance measured as increased plasma levels of glucose, insulin and free fatty acids, and SR-202 protected against these changes.	S1320
T0901317 >98%	LXR agonist whose treatment results in an LXR-dependent up-regulation of ABC1 gene expression	T2320
Tetradecylthioacetic acid ≥97% (NMR)	PPARα agonist; activation in ranking order: PPARα > PPARδ > PPARγ	T1698
Troglitazone >98% (HPLC)	PPARγ agonist; anti-diabetic thiazolidinedione (TZD) with anti-inflammatory and anti-tumor activity; induces apoptosis via a p53 pathway.	T2573
TTNPB	Selective and highly potent retinoic acid analog with affinity for retinoic acid receptors (RAR) α, β, and γ, which are nuclear transcription factors. Produces ligand-activated transcription of genes that possess retinoic acid responsive elements.	T3757
WY-14643	Selective PPARα agonist.	C7081
XCT790 ≥98% (HPLC), solid	XCT790 is a potent and specific inverse agonist of ERRα. XCT790 is selective; showing no significant antagonist activity on related nuclear receptors, such as ERRγ or ERα at concentrations below 10 μM. XCT790 inhibits the constitutive activity of ERRα in both biochemical and cell-based assays. The IC₅₀ value is 300-500 nM in transient transfection assays using GAL4-ERR LBD or full-length ERR with the mSHP promoter.	X4753

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