Metabolism

ICMT-IN-31 (compound 68) serves as an ICMT inhibitor, demonstrating significant potency with an IC50 value of 0.0038 μM [1].

PF-05236216 is a potent, selective, brain-penetrant CK1δ/ε inhibitor that modulates circadian rhythms in mice, supporting sleep and metabolic research.

GNE-618 is a potent and orally active inhibitor of nicotinamide phosphoribosyltransferase (IC50: 6 nM).

Rosuvastatin zinc salt (Rosuvastatin zinc), a zinc-infused variant of Rosuvastatin, functions as an HMG-CoA reductase inhibitor, utilized primarily in

1,2-Distearoyl-3-oleoyl-rac-glycerol, a triacylglycerol, comprises stearic acid at the sn-1 and sn-2 positions and oleic acid at the sn-3 position. This compound is present in cocoa butter and vegetable oils.

1-Palmitoyl-2-oleoyl-3-stearoyl-rac-glycerol, a primary triacylglycerol in cocoa butter, features palmitic acid (at the sn-1 position), oleic acid (at the sn-2 position), and stearic acid (at the sn-3 position).

cis-ent-Tadalafil (cis-ent-IC-351) is a potent and selective PDE5 inhibitor that lowers blood pressure.

1-1(Z)-Hexadecenyl-2-palmitoyl-sn-glycero-3-PE, a plasmalogen, incorporates 1(Z)-hexadecenoic acid and palmitic acid at the sn-1 and sn-2 positions, respectively.

GYKI-16084 is a postsynaptic alpha2 receptor blocker with potential efficacy in the treatment of benign prostatic hyperplasia.

MeIm (compound 7), a peptide mimetic targeting PCSK9, exhibits cholesterol-lowering properties by enhancing the cellular uptake of LDL (EC 50 = 6.04 μM) and obstructing PCSK9's interaction with LDLR (IC 50 = 11.2 μM). This compound is useful for research in cardiovascular diseases.

ICMT-IN-21 (compound 6ag) is an ICMT inhibitor with an IC50 value of 8.8 µM, featuring sulfonamide-modified farnesyl cysteine (SMFC).

N-Acyl taurines, such as N-lignoceroyl taurine, alongside various arachidonoyl amino acid conjugates like N-arachidonoyl dopamine and N-arachidonoyl-L-serine, have been identified in bovine brain and through mass spectrometry lipidomic studies in the brain and spinal cord of both wild-type and FAAH knockout mice. Notably, N-lignoceroyl taurine levels were found to be 23-26 times higher in FAAH knockout mice than in wild types, suggesting its degradation by FAAH, despite in vitro evidence showing FAAH hydrolyzes N-lignoceroyl taurine significantly slower than oleoyl ethanolamide. Additionally, N-acyl taurines with polyunsaturated acyl chains are known to activate TRPV1 and TRPV4 channels within the transient receptor potential (TRP) family of calcium channels.

KD-026 (SLx 4090), a microsomal triglyceride transfer protein (MTP) inhibitor(IC50 = 8.0 nM), is used in type 2 diabetes studies.

IDO-IN-9 is an indoleamine-2,3-dioxygenase (IDO) inhibitor with IC50s of 0.011 μM (Kinase) and 0.0018 μM (Hela Cell).

ICMT-IN-18 (compound 35) serves as an ICMT inhibitor with an IC50 value of 0.066 μM [1].

Branched fatty acid esters of hydroxy fatty acids (FAHFAs) are endogenous lipids that are influenced by fasting and high-fat diets and linked to improved insulin sensitivity in mice. These compounds typically feature a chain of either 16 or 18 carbon atoms (for example, palmitoleic, palmitic, oleic, or stearic acid) esterified with a hydroxy fatty acid chain of similar length. One specific FAHFA, known as 5-OAHSA, consists of oleic acid bonded to the fifth carbon of hydroxy stearic acid. Within the FAHFA family, OAHSAs exhibit the highest serum levels in AG4OX mice, which are known for their glucose tolerance attributed to the overexpression of the Glut4 glucose transporter in adipose tissue.

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

1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.

CLB-016 is an inhibitor of hypoxia-inducible factor (HIF)-1.