Metabolism

1,2-Dioleoyl-3-docosohexaenoyl-rac-glycerol, a triacylglycerol, consists of oleic acid at the sn-1 and sn-2 positions and docosahexaenoic acid at the sn-3 position. This compound has been identified in human breast milk.

Prostaglandin H2 (PGH2), initially isolated from the incubation of arachidonic acid with ovine seminal vesicle microsomes, acts as a potent vasoconstrictor. It serves as the precursor for all 2-series prostaglandins (PGs) and thromboxanes (TXs). Moreover, as a TP receptor agonist, PGH2 irreversibly aggregates human platelets at concentrations of 50-100 ng/ml.

Clocortolone pivalate, a synthetic steroid, treats dermatitis and psoriasis.

LNP Lipid-8 (11-A-M), an ionizable lipid, is utilized in lipid nanoparticles (LNP) for siRNA delivery to T cells without ligand targeting. When loaded with GFP siRNA (siGFP), it significantly silences the GFP gene in a mouse model [1].

CJ-463, a selective uPA blocker, shows strong anti-tumor effect, especially at 100mg/kg, potentially treating lung cancer.

sEH/AChE-IN-4-15 is a dual sEH and AChE inhibitor crossing the BBB, with IC50s: 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE), 14.5 nM (msEH), 102 nM (mAChE).

Mitochondria degrader-1, a potent autophagy inducer, aids in neurodegenerative, cancer, and aging disease research.

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are lipids that are modulated by dietary changes such as fasting and high-fat diets, and they play a role in insulin sensitivity. These compounds generally consist of a fatty acid chain of either 16 or 18 carbons (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified to a similarly long hydroxy fatty acid. One specific FAHFA, 9-SAHSA, features stearic acid esterified at the 9th carbon of hydroxy stearic acid. The concentration of 9-SAHSA is notably increased in the serum of glucose-tolerant AG4OX mice, which specifically express the Glut4 glucose-transporting protein in adipose tissue.

PTP1B-IN-20: Selective PTP1B inhibitor, IC50=1.05μM; less effective on TCPTP (IC50=78μM), targets type 2 diabetes.

BMS-962212: reversible, selective FXIa blocker, well-tolerated, quick PD effect, rapid clearance, alters clotting time/activity.

PHD-IN-2 (Compound 91), a potent PHD antagonist with an IC50 of less than 5 nM, effectively stimulates erythropoietin synthesis in HEP3B cells with an EC50 of

RORγt modulator 4 is a RORγt modulator that regulates IL-17A production activity in cells derived from mouse spleen.

FTI-276 is an inhibitor of protein farnesyltransferase (PFT) (IC50s: 0.9 and 0.5 nM for Plasmodium falciparum and human).

LFHP-1c, a neuroprotective PGAM5 inhibitor, demonstrates efficacy in preserving blood-brain barrier integrity following ischemic stroke.

α-Glucosidase-IN-29 (compound 19) is an inhibitor of α-glucosidases, exhibiting an IC50 value of 1.21 μM and a Ki of 1.80 μM.

C22 Phytoceramide (t18:0/22:0) is a lipid molecule that can be used in life science related research. The CAS number of C22 Phytoceramide (t18:0/22:0) is 164576-03-8.

7,12-Diketolithocholic acid, a bile acid, exhibits elevated plasma levels in patients experiencing cholestasis.

PF-04957325 is an inhibitor of PDE8.PF-04957325 has an IC50 of 0.7 nM for PDE8A.PF-04957325 can be used for the study of autoimmune encephalomyelitis.

MLS000545091 is a potent and selective human epithelial 15-lipoxygenase-2 mixed-type inhibitor.

CYP3A4-IN-2, a potent CYP3A4 inhibitor (IC50: 0.055 μM), is a hydrophobic ritonavir analog with immunosuppressive and antiviral properties.