9(10)-Nitrooleate（NOA）is an endogenous nitrated fatty acid that functions as a highly efficient bioactive molecule. Its primary role is the specific inhibition of the STING protein, a key inflammatory signaling sensor within cells. When STING is aberrantly activated, it can trigger a severe inflammatory response, leading to cellular damage.Mechanistically, NOA acts as an electrophile, capable of covalently modifying specific cysteine residues on the STING protein, thereby effectively blocking its ability to activate downstream signaling pathways. This inhibitory action establishes NOA as a potent endogenous anti-inflammatory agent. In practical application, loading NOA into delivery systems, such as lipid nanoparticles, equips them with an intrinsic "molecular fire extinguisher." It significantly mitigates the acute inflammatory response triggered by delivered cargo, effectively transforming otherwise toxic delivery vehicles into safe platforms. The core value of NOA lies in its ability to provide exceptional safety without compromising the functional expression of therapeutic payloads, offering a crucial safeguard for achieving long-term treatments.

ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research.

12-Nitrolinoleate (12-Nitro-9-cis,12-cis-octadecadienoic acid) is an activator for peroxisome proliferator-activated receptor γ (PPARγ). 12-Nitrolinoleate is a nitrated form of linoleic acid. 12-Nitrolinoleate can be formed upon exposure to acidified nitrate and found in human red blood cells and plasma. 12-Nitrolinoleate can activate PPARγ-dependent gene expression in MCF-7 cells expressing PPARγ with an EC50 = 0.045 μM. 12-Nitrolinoleate is able to inhibit LPS-induced NF-κB transcription in RAW 264.7 cells. 12-Nitrolinoleate can inhibit IL-6, TNF-α and CCL2 induced by LPS.

LCI765 is an orally active and selective PPARδ agonist, with an EC50 of 0.07 nM. LCI765 can be used for the research of diseases related to energy homeostasis such as metabolic syndrome.

KRP-105 is a potent, highly selective, and orally effective PPAR alpha (EC50 = 8 nM) agonist. KRP-105 can significantly reduce serum triglyceride, total cholesterol, and non high density lipoprotein cholesterol levels. KRP-105 can be used for research on metabolic diseases such as dyslipidemia.

(+)-Arhalofenate ((+)-MBX 102) is the less active enantiomer of Arhalofenate. Arhalofenate is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.

NC-2100 is a PPAR activator. NC-2100 can effectively reduce the plasma glucose and triglyceride levels of obese KKAy mice. NC-2100 can induce UCP1 and UCP2 expression in mesenteric and subcutaneous WAT of mice. NC-2100 can be used in research related to type 2 diabetes.

SB-219994 is a peroxisome proliferator-activated receptors (PPARs) agonists. SB-219994 can inhibit airway neutrophilia and associated chemoattractants/survival factors. SB-219994 exhibits anti-inflammation effec.

VSP-77 is an orally active PPARγ agonist. VSP-77 selectively upregulates the expression of insulin sensitivity-related genes (Glut4 and Adiponectin) by inhibiting CDK5-mediated phosphorylation of PPARγ at Ser-273. VSP-77 significantly improves glucose tolerance, reduces fasting blood glucose and insulin levels in high-fat diet (HFD)-induced diabetic mouse models. VSP-77 can be used for the study of diabetes.

8(9)-EET is a major cytochrome P450 (CYP450) metabolite in the renal cortex[1][2]. It activates PPARα in HEK293 cells when used at a concentration of 1 μM but inhibits NF-κB activity induced by IL-1β in a PPARα-dependent and -independent fashion. It is also a substrate of COX-1 and COX-2, as measured by oxygen consumption and product formation assays when used at a concentration of 50 μM .

Deutaleglitazar (Aleglitazar-d2) is a agonist of dual peroxisome proliferatory activating receptor (PPARα and PPARγ).

GW9820 is PPARα and PPARγ activator (EC50s: 0.37 μM for PPARα; 0.288 μM for PPARγ). GW9820 increases CLA-1. GW9820 can be used in the research of atherosclerosis.

SP-C01 is an orally active soluble epoxide hydrolase (sEH) inhibitor and partial PPARγ agonist. SP-C01 can inhibit Ser273 phosphorylation.

SKLB102 shows a high affinity with PPARγ. SKLB102 has potent ability to reduce fat deposition and protect liver against non-alcoholic fatty liver disease (NAFLD) through regulating adipocytokine expression and preventing insulin resistance.

PT-S58, a GSK0660 derivative, is a PPARβ/δ full antagonist with an IC50 value of 98 nM. PT-S58 inhibits the agonist-induced transcriptional activity of PPARβ/δ in vitro.

MHY 553 is a PPARα agonist that is effective when taken orally. MHY 553 helps alleviate liver fat accumulation by increasing fatty acid oxidation and reducing inflammation during the aging process. MHY 553 inhibits the accumulation of triglycerides induced by liver X receptor agonists in HepG2 cells. MHY 553 significantly suppresses the expression of inflammatory mRNA in aging rats.

E0924G is an orally active activator for PPARδ with EC50 of 2.82 μM. E0924G promotes the upregulation of osteoprotegerin (OPG) with an EC50 of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibites F-actin ring formation in RAW264.7 macrophages. E0924G regulates the bone density and bone loss in ovariectomized (OVX) and age-related osteoporosis models.

DN-108, a thiazolidinedione derivative, is an orally active peroxisome proliferator-activated receptor γ (PPARγ) agonist with antidiabetic effects. DN-108 improves hyperglycemia, hypertriglyceridemia and hyperinsulinemia in diabetic mouse models. DN-108 enhances tissue glucose uptake (e.g., increasing 2-deoxyglucose uptake in L6 muscle cells) and inhibits fatty acid synthase activity. DN-108 is promising for research of type 2 diabetes.

Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively.

Apo-12'-lycopenal is a Lycopene metabolite. Apo-12'-lycopenal promotes adipocyte differentiation and adiponectin secretion via PPAR-γ activation.

Amezalpat is the antagonist for PPARα with IC50 of 58 nM. Amezalpat exhibits antineoplastic activity.

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.

(E)-CLX-0921 is the E-isomer of CLX-0921 with antiviral activity. 5-Oxo leukotriene B4 is promising for research of viral infections caused by human and animal enveloped RNA viruses.

(±)-CBCQ is an oxidative product of cannabichromene, with an EC50 of 14.7 μM for PPAR-γ.

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.

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.

GW0742 is a potent PPARβ and PPARδ agonist, with an IC50 of 1 nM for human PPARδ in binding assay, and EC50s of 1 nM, 1.1 μM and 2 μM for human PPARδ, PPARα, and PPARγ, respectively.

Seladelpar is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist.

Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α (PPAR-α) and peroxisome proliferator-activated receptor-δ (PPAR-δ) with EC50 values of 45 and 175 nM, respectively.

2,4-Thiazolidinedione (Thiazolidinedione), an insulin sensitizer, is a specific agonist of peroxisome proliferator-activated receptor (PPAR)γ. Thiazolidinedione treatment corrects impaired muscle insulin action in vivo.