Metabolism

Trolox is an antioxidant like vitamin E and it is used to reduce oxidative stress or damage.

SR 18292 is a PGC-1α inhibitor. It reduces blood glucose, strongly increases hepatic insulin sensitivity, and improves glucose homeostasis in dietary and genetic mouse models of T2D.

3-methoxy Tyramine (HCl) is a natural metabolite of dopamine, produced by catechol-O-methyltransferase (COMT).

CAY10566 is a potent and selective inhibitor of SCD1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.

IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.

Tropifexor, also known as LJN452, is a farnesoid X receptor agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

Oxyclozanide is a salicylanilide anthelmintic that is a proton ionophore which uncouples oxidative phosphorylation of the target organism.

Valpromide is an amide derivative of valproic acid and inhibits human epoxide hydrolase.

Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi.

Roflumilast N-oxide is the active metabolite of roflumilast. Roflumilast N-oxide is a phosphodiesterase 4 inhibitor.

Glutathione oxidized, or GSSG, results from glutathione undergoing oxidation. It plays a crucial role in neutralizing reactive oxygen species, a process that concurrently generates GSSG. This oxidized form of glutathione is pivotal in studies concerning sickle cells and erythrocytes, where it's utilized for research purposes.

Ethoxyquin is an antioxidant that is widely used in animal feed to protect against lipid peroxidation and fat rancidity in chicken, salmon, and beef.

PX20606, also known as PX-102, is a FXR agonist. It induces high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice.

Px-104, also known as Px-102, is a farnesoid X receptor (FXR) agonist potentially for the treatment of non-alcoholic fatty liver disease.

Diaveridine (EGIS-5645) is a dihydrofolate reductase (DHFR) inhibitor with a Ki of 11.5 nM for the wild type DHFR and also an antibacterial agent.

BRL-50481 acts as a phosphodiesterase inhibitor selective for the PDE7 subtype.

BMS-986205, also known as Linrodostat, ONO-7701 and F001287, a potent and selective, orally active IDO1 inhibitor with potential immunomodulating and antineoplastic activities. CAS: 1923833-60-6 (free base) 2221034-29-1 (mesylate)

LY2562175 is a potent and selective FXR agonist in vitro and has robust lipid modulating properties, lowering LDL and triglycerides while raising HDL in preclinical species.

GSK-2033 is a potent cell-active LXR antagonist (pIC50 = 7.5). It enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells and is cell permeable.

BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor.

LTI-291 is a glucocerebrosidase (Gcase) activator for treatment of Parkinson's disease (PD).

Lanifibranor, also known as IVA-337, is a peroxisome proliferator-activated receptors (PPAR) agonist.

Androsterone is a steroid hormone produced in the body from 5α-reduced metabolites of dehydroepiandrosterone. It is the major androgen excreted in urine as a metabolite of testosterone and is used as the international reference standard for androgenic activity.

BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1).

Alagebrium Chloride, also known as ALT711, was the first drug candidate to be clinically tested for the purpose of breaking the crosslinks caused by advanced glycation endproducts (AGEs), thereby reversing one of the main mechanisms of aging.

1-Linoleoyl glycerol (1-LG) is a fatty acid glycerol that has been isolated from S. chinensis roots. It inhibits PAF-AH with an IC50 of 45 μM.

Menaquinone-4 is a vitamin K, used as a hemostatic agent, and also a adjunctive therapy for the pain of osteoporosis.

Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM.

BW-A78U is a PDE4 inhibitor with an IC50 of 3 μM.

Timegadine, a new antiinflammatory agent, is found to be a potent, competitive inhibitor of cyclo-oxygenase (COX) and lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit platelets) to 20 μM (rat brain) for COX and 100 μM for lipo-oxygenase both in the cytosol fraction of horse platelet homogenates, and in washed rabbit platelets.

SGC GAK 1 is a high affinity cyclin G associated kinase (GAK) inhibitor.

NCT-503 is an inhibitor of 3-phosphoglycerate dehydrogenase (PHGDH) with an IC50 value of 2.5 μM.

HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1).

E6446 dihydrochloride is a robust antagonist for TLR7 and TLR9, with potential applications in studying harmful inflammatory responses. Additionally, it acts as a significant inhibitor of SCD1 with a KD of 4.61 μM. This compound can notably suppress adipogenic differentiation and liver lipogenesis via the SCD1-ATF3 pathway. Studies have indicated that E6446 dihydrochloride can enhance liver pathology in mice on a high-fat diet, making it a potential candidate for researching non-alcoholic fatty liver disease (NAFLD).

TRC051384 hydrochloride is an inducer of heat shock protein Hsp70.

UK-371804 is a potent urokinase-type plasminogen activator (uPA) inhibitor.

BIA10-2474 is a long-acting reversible inhibitor of fatty acid amide hydrolase (FAAH) .

COH29 is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity.

AMG-333 is a potent and selective TRPM8 Antagonist.

Eltanexor, also known as KPT-8602, is a second-generation exportin-1 inhibitor.

AZ-PFKFB3-67 is a novel potent and selective PFKFB3 inhibitor.

BAY-876 is a potent and Selective GLUT1 Inhibitor. BAY-876 showed good metabolic stability in vitro and high oral bioavailability in vivo.

PUN30119, also known as Imidazole ketone erastin (IKE), is a potent, metabolically stable inhibitor of system xc- and inducer of ferroptosis potentially suitable for in vivo applications.

KL1333 is an orally available, small organic molecule that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL-1333 Improves Energy Metabolism and Mitochondrial Dysfunction in MELAS Fibroblasts.

E260 is a novel inhibitor of the Fer/FerT kinase with Kd of 0.85 uM.

Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release.

Tauroursodeoxycholate (TUDCA; UR 906; Taurolite) is an endoplasmic reticulum (ER) stress inhibitor.

Thymopentin is a synthetic pentapeptide corresponding to the amino acids 32-36 of thymopoietin and exhibiting the full biological activity of the natural hormone. It is an immunomodulator which has been studied for possible use in the treatment of rheumatoid arthritis, AIDS, and other primary immunodeficiencies.

Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9.

D-α-Tocopherol acetate (D-Vitamin E acetate) can be hydrolyzed to d-alpha-tocopherol (VE) and absorbed in the small intestine.