PPAR Agonists and Antagonists

A1120
This is a selective non-retinoid ligand for retinol-binding protein 4 (RBP4). RBP4 transports retinol from the liver to extrahepatic tissues.
Katalog # CAS Nummer Summenformel Menge
sc-300151 n.n. C₂₀H₁₉F₃N₂O₃ 25 mg
AC-41848 hydrate
A potent, cell permeable, subtype selective retinoic acid receptor RAR agonist. AC-41848 has high selectivity (92%) for RAR . EC₅₀= 5.9 µM.
Katalog # CAS Nummer Summenformel Menge
sc-252347 400856-69-1 (anhydrous) C₂₁H₂₁BrCl₂N₂ ·xH₂O 5 mg
AC 264613
AC 264613 is a selective and potent protease-activated receptor 2 (PAR2) agonist.
Katalog # CAS Nummer Summenformel Menge
sc-358026 1051487-82-1 C₁₉H₁₈BrN₃O₂ 10mg/50mg
AM3102
Oleoyl ethanolamide (OEA) is an endogenous agonist for proliferator-activated receptor α (PPARα) that promotes lipolysis, suppresses food intake, and reduces weight gain in rodents. The biological effects of OEA are terminated by N-acylethanolamine-hydrolyzing acid amidase and fatty-acid amide hydrolase. AM3102 is an OEA analog that stimulates PPARα transcriptional activity with an EC₅₀ value of 100 nM and prolongs feeding latency in rodents with an ED₅₀ value of 2.4 mg/kg. It is resistant to enzymatic hydrolysis and is as potent as OEA in reducing food intake in free-feeding rats and enhancing transcriptional activity of PPARα. AM3102 demonstrates weak affinity for the peripheral cannabinoid (CB2) and central cannabinoid (CB1) receptors with Ki values of 26 and 33 µM, respectively.
Katalog # CAS Nummer Summenformel Menge
sc-223774 213182-22-0 C₂₁H₄₁NO₂ 5 mg/10 mg
BADGE
An inhibitor of the peroxisome proliferator-activated receptor (PPAR)-γ and adipocyte differentiation, and has been shown to induce apoptosis in tumor cells.
Katalog # CAS Nummer Summenformel Menge
sc-202487 1675-54-3 C₂₁H₂₄O₄ 25 g
CAY10506
Anti-diabetic drugs of the thiazolidinedione (TZD) structural class as well as α-lipoic acid activate peroxisome proliferator-activated receptor γ (PPARγ), a nuclear transcription factor that controls lipid homeostasis and glucose metabolism. CAY10506 is a hybrid lipoic acid-TZD derivative that trans-activates human PPARγ with an EC₅₀ value of 10 µM.
Katalog # CAS Nummer Summenformel Menge
sc-221403 292615-75-9 C₂₀H₂₆N₂O₄S₃ 1 mg/5 mg
CAY10599
Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo. The prototypical compound for this class is the TZD rosiglitazone (BRL 49653), which is currently marketed for diabetes treatment. CAY10599 is a PPARγ agonist that is 4-fold more potent than rosiglitazone at PPARγ demonstrating an EC₅₀ value of 0.05 µM. This compound shows high selectivity for the PPARγ receptor over PPARδ (EC₅₀ > 10 µM) or PPARα (EC₅₀ = 3.99 µM).
Katalog # CAS Nummer Summenformel Menge
sc-223876 1143573-33-4 C₃₈H₄₁NO₅ 1 mg/5 mg
CP 775146
Katalog # CAS Nummer Summenformel Menge
sc-361158 702680-17-9 C₂₆H₃₃NO₄ 10 mg/50 mg
DRF 2519
DRF-2519 is a dual PPARα/γ activator. It has better reduction of plasma insulin, triglyceride, and free fatty acid levels than those treated with rosiglitazone.
Katalog # CAS Nummer Summenformel Menge
sc-300504 n.n. C₂₀H₁₈N₂O₅S 25 mg
(+)-Etomoxir sodium salt hydrate
PPARα activator; Irreversible O-carnitine palmitoyltransferase-1 (CPT-1) inhibitor
Katalog # CAS Nummer Summenformel Menge
sc-215009 828934-41-4 (anhydrous) C₁₅H₁₈ClO₄ ·Na ·H₂O 5 mg/25 mg
GSK 0660
Selective PPARδ antagonist (IC₅₀ values are 0.155, > 10 and ≥ 10 μM at PPARδ, PPARα and PPARγ respectively). Exhibits inverse agonist effects when administered by itself.
Katalog # CAS Nummer Summenformel Menge
sc-203985 1014691-61-2 C₁₉H₁₈N₂O₅S₂ 10 mg/50 mg
GSK 3787
A selective PPARδ (peroxisome proliferator-activated receptor δ) antagonist which binds to Cys249 in the PPARδ binding pocket.
Katalog # CAS Nummer Summenformel Menge
sc-358241 188591-46-0 C₁₅H₁₂ClF₃N₂O₃S 10mg/50mg
GSK4112
GSK4112 is s reverb agonist. It is the first known agent able to reset the circadian clock in a phase-dependent manner.
Katalog # CAS Nummer Summenformel Menge
sc-300774 n.n. C₁₈H₂₁ClN₂O₄S 5 mg/10 mg
GW 0742
A PPARβ ligand that has been shown to activate PPARβ. Has also been reported to enhance the expression of interleukin IL-6 and IL-8.
Katalog # CAS Nummer Summenformel Menge
sc-203991 317318-84-6 C₂₁H₁₇F₄NO₃S₂ 10 mg/50 mg
GW 1929
A potent, tyrosine-based peroxisome proliferator-activated receptor γ (PPARγ) agonist (EC₅₀ = 13 nM for murine receptor and 6.2 nM for human receptor in cell-based transactivation assays).
Katalog # CAS Nummer Summenformel Menge
sc-202640 196808-24-9 C₃₀H₂₉N₃O₄ 1 mg
GW 7647
Shown to be a potent PPARα agonist with 200-fold selectivity over PPARγ and PPARδ. Also been found to cause an up-regulation of β-oxidation gene expression.
Katalog # CAS Nummer Summenformel Menge
sc-203068 265129-71-3 C₂₉H₄₆N₂O₃S 5 mg
GW1929 hydrate
GW1929 is a high affinity agonist of PPAR-γ.
Katalog # CAS Nummer Summenformel Menge
sc-300778 196808-24-9 (anhydrous) C₃₀H₂₉N₃O₄•xH₂O 5 mg
GW501516
Specific agonist for PPARδ (EC₅₀=1.1nM) with a 1'000-fold selectivity over the other human subtypes.
Katalog # CAS Nummer Summenformel Menge
sc-202642 317318-70-0 C₂₁H₁₈F₃NO₃S₂ 1 mg/5 mg
GW6471
GW6471 is a PPARα antagonist, shown to completely inhibit GW409544-induced activation of PPARα.
Katalog # CAS Nummer Summenformel Menge
sc-300779 436159-64-7 C₃₅H₃₆F₃N₃O₄ 5 mg
L-165041
A peroxisome cell permeable proliferator-activated receptor δ (PPARδ) agonist which induces adipocyte differentiation in NIH-PPARδ cells.
Katalog # CAS Nummer Summenformel Menge
sc-203094 79558-09-1 C₂₂H₂₆O₇ 5 mg
LY 171883
A leukotriene D4 antagonist that has been shown to displace oleic acid binding to FABPs. Reported to contain structural similarity to fatty acids.
Katalog # CAS Nummer Summenformel Menge
sc-203120 88107-10-2 C₁₆H₂₂N₄O₃ 10 mg
Methyl-8-hydroxy-8-(2-pentyl-oxyphenyl)-oct-5-ynoate
An aromatic analog of 8(S)-HETE that acts as a dual agonist of PPARα and PPARγ with EC₅₀ values of 0.173 and 0.642 µM, respectively.
Katalog # CAS Nummer Summenformel Menge
sc-204803 868526-38-9 C₂₀H₂₈O₄ 1 mg/5 mg
Muraglitazar
A peroxisome proliferator-activated receptor (PPAR) α/γ dual agonist.
Katalog # CAS Nummer Summenformel Menge
sc-211931 331741-94-7 C₂₉H₂₈N₂O₇ 1 mg
NPC 15199
An N-FMOC-protected leucine compound with antiinflammatory effects. A chemically distinct modulator of PPARγ. Demonstrated to increase intracellular Ca²⁺ and to mobilize Ca²⁺ stores in human BFTC cells.
Katalog # CAS Nummer Summenformel Menge
sc-202741 35661-60-0 C₂₁H₂₃NO₄ 250 mg
nTZDpa
A selective non-thiazolidinedione PPARγ agonist, that does not affect PPARα or PPARδ receptors. This compound has been shown to regulate adipocyte development and gene expression.
Katalog # CAS Nummer Summenformel Menge
sc-204140 118414-59-8 C₂₂H₁₅Cl₂NO₂S 10 mg/50 mg
PAz-PC
Potent PPARγ receptor agonist which competes for the thiazoladinedione binding site. More potent than 15-deoxy-Δ12,14-prostaglandin J2; equipotent with rosiglitazone as a ligand for this receptor.
Katalog # CAS Nummer Summenformel Menge
sc-202757 117205-52-4 C₃₃H₆₄NO₁₀P 1 mg/5 mg
Pioglitazone
Shown to be a PPARγ1 and PPARα activator. In vitro it has been noted that this agent promotes adipocyte differentiation of mesenchymal and preadipocyte stem cell lines.
Katalog # CAS Nummer Summenformel Menge
sc-202289 111025-46-8 C₁₉H₂₀N₂O₃S 1 mg/5 mg
Rosiglitazone
A potent, selective PPARγ agonist which exhibits anti-diabetic and hepatoxic effects. Increases insulin sensitivity in muscle and adipose tissue, and plays a functional role in adipogensis.
Katalog # CAS Nummer Summenformel Menge
sc-202795 122320-73-4 C₁₈H₁₉N₃O₃S 25 mg/100 mg
Rosiglitazone (potassium salt)
A peroxisome proliferator-activated subtype gamma receptor (PPARγ) agonist which regulates the epithelial sodium channel (ENaC) and Na-K-2Cl (NKCC2) co-transporter.
Katalog # CAS Nummer Summenformel Menge
sc-205493 316371-84-3 C₁₈H₁₈N₃O₃S ·K 5 mg/10 mg
Rosiglitazone-d3 Maleate
An anti-diabetic drug from the thiazolidinedione class; a selective ligand of PPARγ, that has no PPARα-binding action.
Katalog # CAS Nummer Summenformel Menge
sc-224260 155141-29-0 C₂₂H₁₈D₅N₃O₇S 1 mg/5 mg
S26948
Katalog # CAS Nummer Summenformel Menge
sc-361331 353280-43-0 C₂₈H₂₅NO₇S 10 mg/50 mg
SR 202
Attenuates troglitazone-induced PPARγ transcriptional activity. Selective PPARγ antagonist; antidiabetic and antiobesity agent. In vitro and in vivo, inhibits PPARγ -dependent adipocyte differentiation. Also improves insulin sensitivity in diabetic ob/ob mice and increases HDL levels in rats, in vivo.
Katalog # CAS Nummer Summenformel Menge
sc-203700 76541-72-5 C₁₁H₁₇ClO₇P₂ 10 mg
Thiazolidinedione derivative
Katalog # CAS Nummer Summenformel Menge
sc-358842 n.n. C₁₆H₁₃NO₃S₂ 5 mg/10 mg
WY 14643
A highly potent PPARα agonist. Shown to inhibit TNF-α-induced VCAM-1, and reduce TNF-α and IL-1β.
Katalog # CAS Nummer Summenformel Menge
sc-203314 50892-23-4 C₁₄H₁₄ClN₃O₂S 50 mg