Metabolism

(Rac)-8-Hydroxy-efavirenz is a metabolite of Efavirenz, a non-nucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV-1.

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.

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).

LEQ803 (N-DesmethylRibociclib) is a metabolite of the CDK4/6 inhibitor Ribociclib, produced through metabolism by CYP3A4. This compound holds potential applications in the field of oncology.

ATX inhibitor 22 is a novel inhibitor of ATX (autotaxin) (IC50: 218.9 μM) that lacks inhibitory activity against LPAR1.

Falecalcitriol is an analog of calcitriol. It has a higher potency both in vivo and in vitro systems, which is longer duration of action in vivo.

(2S,4S)-Sacubitril (Sacubitril Impurity C) is a stereoisomer derived from Sacubitril which is a potent NEP inhibitor.

<p>TNP-470 is a methionine aminopeptidase-2 inhibitor. TNP-470 is also an angiogenesis inhibitor.</p>

DSM705 hydrochloride: potent antimalarial, pyrrole-based DHODH inhibitor effective against Plasmodium, non-toxic to mammalian DHODH.

SMase-IN-1 (Compound 4) is a bacterial sphingomyelinase (SMase) inhibitor with an IC50 value of 6.43 µM against Bacillus cereus SMase. It also inhibits eqBuChE with an inhibition rate of 59.50% at a concentration of 50 µM. SMase-IN-1 forms a complex with Cu2+ through bio-metal interactions and can inhibit hemolysis of sheep red blood cells induced by Bacillus cereus.

GW461484A is a small molecule inhibitor targeting Candida albicans Yck2, exhibiting an IC50 of 0.11 µM. It has a MIC80 of 12.5 µM against C. albicans. GW461484A shows potential for research into fungal diseases, including drug-resistant Candida infections.

(3S,17S)-FD-895 is an analogue of FD-895. It inhibits the growth of HCT116 cells and shows splicing-modulating activity. This compound can be utilized in cancer research.

CK1δ-IN-8 (Compound 429) is a CK1δ inhibitor suitable for Alzheimer's disease research.

Casein kinase1δ-IN-30 (Compound 581) is an inhibitor of casein kinase 1δ (CK1δ). It can be utilized in research related to neurodegenerative diseases.

BT-114143 is a plasminogen activator inhibitor with an IC50 of 8.42 μM. It is applicable in research related to hemorrhagic diseases caused by excessive fibrinolysis, including traumatic bleeding, severe menorrhagia, postpartum hemorrhage, and complications of hemophilia.

LDHA-IN-5 is a novel and potent inhibitor targeting both glycolate oxidase (GO) and lactate dehydrogenase A (LDHA), designed for the treatment of primary

FTI-2148 blocks RAS-related FT-1 & GGT-1; IC50: 1.4 nM & 1.7 μM.

DPM-1003 is an allosteric inhibitor of PTP1B, targeting the non-catalytic, disordered C-terminal segment of the PTP1B protein, and has shown beneficial effects in reducing pulmonary inflammation in mice.

Propofolsulfate (sodium) is a metabolite of Propofol.

BMS-185354 is a selective RARγ activator with an EC50 value of 28 nM, offering potential for cancer research.