| DC9602 |
Balaglitazone
Featured
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Balaglitazone (DRF-2593; NN-2344) is a novel partial agonist of PPAR-γ. |
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| DC28072 |
Mifobate
Featured
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Mifobate (SR-202) is a potent and specific PPARγ antagonist. Mifobate (SR-202) selectively inhibits Thiazolidinedione (TZD)-induced PPARγ transcriptional activity (IC50=140 μM). Mifobate (SR-202) does not affect basal or ligand-stimulated transcriptional activity of PPARα, PPARβ, or the farnesoid X receptor (FXR). Mifobate (SR-202) shows antiobesity and antidiabetic effects. |
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| DC28242 |
15-Deoxy-Δ-12,14-prostaglandin J2
Featured
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15-Deoxy-Δ-12,14-prostaglandin J2 (15d-PGJ2) is a cyclopentenone prostaglandin and a metabolite of PGD2. 15-Deoxy-Δ-12,14-prostaglandin J2 is a selective PPARγ (EC50 of 2 µM) and a covalent PPARδ agonist. 15-Deoxy-Δ-12,14-prostaglandin J2 promotes efficient differentiation of C3H10T1/2 fibroblasts to adipocytes with an EC50 of 7 μM. |
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| DC28684 |
iRucaparib-AP6 |
iRucaparib-AP6 is a highly efficient and specific PARP1 degrader based on Rucaparib by using the
PROTAC approach. iRucaparib-AP6, a non-trapping PARP1 degrader, blocks both the catalytic activity and scaffolding effects of PARP1. |
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| DC29028 |
LY518674 |
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis. |
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| DC40032 |
GSK376501A |
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus. |
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| DC40541 |
Mesalamine impurity P |
Mesalamine impurity P is an impurity of Mesalamine. 5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.
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| DC40731 |
Ciprofibrate impurity A |
Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha. |
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| DC41439 |
Methyl oleanonate |
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects. |
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| DC41468 |
Caulophyllogenin |
Caulophyllogenin is a triterpene saponin extracted from M. polimorpha. Caulophyllogenin is a partial PPARγ agonist, with an EC50?of?12.6?μM. Caulophyllogenin can be used for the research of type-2 diabetes, obesity, metabolic syndrome and inflammation. |
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| DC45608 |
FK614 |
FK614 is an orally active, potent, selective PPARγ modulator (SPPARM). FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 is a nonthiazolidinedione insulin sensitizer. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes. |
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| DC46878 |
AMG131 |
AMG131 (INT131), a potent and highly selective PPARγ partial agonist, binds to PPARγ and displaces Rosiglitazone with a Ki of ~10 nM. AMG131 can be used for research of type-2 diabetes mellitus (T2DM). |
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| DC46879 |
(S)-Coriolic acid |
(S)-Coriolic acid (13(S)-HODE), the product of 15-lipoxygenase (15-LOX) metabolism of linoleic acid, functions as the endogenous ligand to activate PPARγ. (S)-Coriolic acid is an important intracellular signal agent and is involved in cell proliferation and differentiation in various biological systems. (S)-Coriolic acid induces mitochondrial dysfunction and airway epithelial injury. |
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| DC47176 |
GW 590735
Featured
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GW 590735 is a potent and selective PPARα agonist. GW 590735 showsEC50=4 nM on PPARα and at least 500-fold selectivity versus PPARδ and PPARγ. GW 590735 can be used for the research of dyslipidemia. |
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| DC48265 |
Vutiglabridin |
Vutiglabridin is a synthetic structural analog of glabridin for the treatment of obesity. |
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| DC48266 |
Rivoglitazone |
Rivoglitazone is a thiazolidinedione-derivative PPARγ agonist for the treatment of type 2 diabetes mellitus. |
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| DC48267 |
Farglitazar |
Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients. |
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| DC48268 |
KRP-297 |
KRP-297 is a PPARα and PPARγ agonist potentially for the treatment of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver. |
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| DC48269 |
Ragaglitazar |
Ragaglitazar is a PPARα and PPARγ agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models. Ragaglitazar improves glycemic control and lipid profile in type 2 diabetic. |
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| DC48270 |
Bocidelpar
Featured
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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). |
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| DC48271 |
10-Nitrolinoleic acid |
10-Nitrolinoleic acid is a potent peroxisome proliferator-activated receptor γ (PPARγ) agonist. 10-Nitrolinoleic acid competes with [3H]Rosiglitazone for binding to PPAR-γ, with an IC50 of 0.22 μM. |
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| DC49825 |
SR2595 |
SR2595 is an inverse agonist of PPARγ with an IC50 of 30 nM. |
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| DC49826 |
AZD-9574
Featured
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AZD9574 is a CNS-penetrant, PARP1-selective inhibitor with IC50 of <0.005 μM. AZD9574 demonstrates >10,000-fold selectivity for PARP1 over PARP2 and shows excellent preclinical PK acrossseveral species, with low clearance and high oral bioavailability, and demonstrated in vivo efficacy in a BRCA2−/− DLD-1 mouse xenograft model. |
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| DC49827 |
PPARα/δ agonist 1 |
PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis. |
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| DC70669 |
NXT629 |
NXT629 (NXT-629) is a potent, selective PPARα antagonist with IC50 of 77 nM (human PPARα), no effect against PPARδ and PPARγ (IC50>30 uM).NXT629 inhibited agonist-induced transcription of PPARα-regulated genes, demonstrating target engagement in chronic lymphocytic leukemia (CLL) cells.NXT629 induced apoptosis of CLL cells even in the presence of a protective microenvironment.NXT629 reduces the number of chronic leukemia cells undergoing cell division with IC50 of 9.6 uM.NXT629 reduces CLL tumor burden delays disease progression of CLL in CLL mouse model. |
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| DC70704 |
PPARγ pSer273-IN-10 |
PPARγ pSer273-IN-10 is a specific, in vivo-active small molecule inhibitor of CDK5-mediated Ser273 phosphorylation of PPARγ without classical PPARγ agonism.PPARγ pSer273-IN-10 is a potent PPARγ binder and in vitro inhibitor of the CDK5-mediated phosphorylation of PPARγ Ser273 and displays negligible PPARγ agonism in a reporter gene assay. PPARγ pSer273-IN-10 demonstrated an improvement in insulin sensitivity in the ob/ob diabetic mouse model in 7 day treatment in vivo testing. |
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| DC70905 |
WO95E |
WO95E is a novel potent, synthetic ligand (partial agonist) of PPARγ, directly binds to PPARγ with IC50 of 11 nM;
WO95E's binding affinity is approximately 70-fold lower than that of UHC1 (Journal of Biological Chemistry. 2014;289(38):26618–26629.).
WO95E significantly inhibited the S273 phosphorylation of PPARγ in 3T3-L1 differentiated adipocytes, led to the upregulation of the mRNA levels of a number of the PPARγ phosphorylation-dependent genes, including adiponectin, cycp2f2, Ddx-17, Rarres2, and Selenbp1.
Unlike SR1664 and UHC1, WO95E does not bind to the canonical PPARγ ligand-binding pocket (LBP) containing H3, H3-4 loop, H11 and H12, which full agonist Rosi binds, instead, WO95E binds to the ABP comprising H2′-H3, β-sheet, and the Ω loop.
WO95E improved glucose tolerance and insulin sensitivity in DIO mice. |
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| DC71112 |
S26948 |
S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ. |
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| DC71195 |
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. |
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| DC71197 |
H-Trp-Glu-OH |
H-Trp-Glu-OH is a selective, reversible and cell-permeable PPARγ with a Kd of ~8 µM. H-Trp-Glu-OH might be developed as a possible lead compound in diabetes research. |
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