Metabolism

EB-0176: A valerian derivative; broad-spectrum antiviral; potent ER α-glucosidase I/II inhibitor; IC50s: 0.6439/0.0011 μM.

BAY-179 is a potent, selective, species cross-reactive complex I inhibitor for the study of cancer.

α-Glucosidase-IN-14 is a potent inhibitor of α-glucosidase (IC50: 5.22 μM).

FXIa-IN-6: Potent, selective FXIa inhibitor (Ki=0.3 nM); strong PK with high oral bioavailability, low clearance preclinically.

Vimirogant (VTP-43742) HCl: Oral, selective RORγt inhibitor (IC50: 17 nM, Ki: 3.5 nM), >1000x selectivity over RORα/β, targets Th17, not Th1/2/Treg.

PF-00489791 (PF4634817) is a long-acting PDE5 inhibitor with hypotensive activity for the study of diabetic nephropathy.

JTT-553 is a DGAT1 inhibitor with an IC50 of 2.38 nM. It effectively reduces plasma levels of glucose, insulin, non-esterified fatty acids (NEFA), total cholesterol (TC), and liver triglycerides (TG). JTT-553 enhances insulin-dependent glucose absorption and glucose intolerance in the adipose tissue of diet-induced obese (DIO) mice. In KK-Ay mice, it lowers TNF-α mRNA levels and elevates GLUT4 mRNA levels in adipose tissue. By contributing to weight loss, JTT-553 improves insulin resistance in adipose tissue and overall glucose metabolism. This compound is useful for research on obesity and type 2 diabetes mellitus (T2DM).

DGAT2-IN-3 (compound 9) is an inhibitor of DGAT2 with an IC50 value of 0.4 nM. It is utilized in research related to fatty liver disease, diabetes, and cardiovascular diseases.

The compound 3,3'-[Dithiobis[2,1-ethanediyl(methylimino)]]bis[1-propanol] is an SS-cleavable, proton-activated lipid-like substance (SSPalm) that facilitates the delivery of plasmid DNA.

Calcipotriol Impurity C is the impurity of Calcipotriol. Calcipotriol is a VDR-like receptors ligand.

AZ513 is a reversible FAAH inhibitor, exhibiting an IC50 of 551 nM for human FAAH and 27 nM for rat FAAH. It inhibits the hydrolysis of arachidonoyl ethanolamide in HEK293 cells transfected with human FAAH, with an IC50 of 360 nM.

SGK1-IN-6 (compound 12f) is an SGK1 inhibitor with an IC50 value of 0.39 μM. In PC3 xenograft models using BALB/c nude mice, SGK1-IN-6 effectively hinders tumor growth without causing any observable toxicity.

QGC583 is an effective and selective AminopeptidaseA (APA) inhibitor, demonstrating an IC50 of 4 nM. It inhibits APA activity in the brain, kidneys, and heart of rats.

P5SA-2 is a selective allosteric activator of PPP5C, functioning by modulating the structure of the PPP5C phosphatase domain. At a concentration of 100 μM, it can enhance PPP5C activity by 3.2-fold, with an apparent affinity constant of 7.8 μM. P5SA-2 is applicable in research related to cancer and Alzheimer's disease.

Homodestcardin: cyclic depsipeptide from T. roseum with immunosuppressant properties; inhibits mouse T cell proliferation.

MAGL-IN-18 (compound 118) serves as a highly potent inhibitor of Monoacylglycerol lipase (MAGL), demonstrating an IC 50 value of 0.03nM.

ACLY Inhibitor 7 is a potent, selective hACLY inhibitor (IC50<1 nM) for metabolic disease and oncology research.

RORγt Inhibitor 2, a potent inhibitor of RORγt, exhibits an IC50 of 9.2 nM and is utilized in the study of cancer, inflammation, or autoimmune diseases that are