lipophilic

Laurocapram (N-Lauryl caprolactam) is a percutaneous enhancer. Upon application to the skin, laurocapram interacts with lipids in the stratum corneum and may enhance the ability of the skin to absorb a hydrophilic chemical.

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

Elesclomol (STA-4783) is an oxidative stress inducer and a highly lipophilic copper ion carrier. Elesclomol induces apoptosis in tumor cells and is used in copper death related studies. Elesclomol also inhibits FDX1-mediated Fe-S cluster biosynthesis.

SBE-β-CD (Sulfobutylether-β-Cyclodextrin) is a β-cyclodextrin derivative with a sodium sulfonate salt separated from the lipophilic cavity by a butyl ether spacer group, or sulfobutylether. SBE-β-CD is widely used as a co-solvent in biological experiments.

Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor (Ki: 0.18 μM) that inhibits estrogen biosynthesis, exhibits antifertility effects, and induces impairment of spatial memory.

Tenifatecan (SN2310) is a highly lipophilic preparation of 7-ethyl-10-hydroxycamptothecin (SN) with potential antitumor activity.

NITD-916 is an orally active and highly lipophilic inhibitor of Mycobacterium enoyl reductase InhA with an IC50 of 570 nM.NITD-916 is a potent 4-hydroxy-2-pyridone derivative that forms a ternary complex with InhA and NADH, preventing access to the fatty acyl substrate-binding pocket.NITD-916 exhibits antituberculosis activity.

Eclazolast (RHC 2871) is a lipophilic anti-allergic compound that inhibits mediator release in a mast cell model.Eclazolast inhibits extracellular secretion by affecting only the direct processes associated with Fc(epsilon)RI in the cell.The effect of Eclazolast is highly dependent on the concentration of antigen that triggers the cell.

JHU395 is an orally-bioavailable prodrug of a lipophilic glutamine antagonist (GA), 6-diazo-5-oxo-L-norleucine (DON). It demonstrates delivery of DON to malignant peripheral nerve sheath tumor (MPNST) both in vitro and in vivo, resulting in significant antitumor activity in MPNST. Additionally, JHU395 exhibits plasma stability.

Sorbitan monooleate is a pharmaceutical excipient, a lipophilic nonionic surfactant, and is often used as an emulsifier in cosmetics, food and pharmaceuticals.

Lufenuron (Fluphenacur) is a chitin-synthesis inhibitor.

Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure.

Baclofen (Lioresal) is a synthetic chlorophenyl-butanoic acid derivative used to treat spasms due to spinal cord damage and multiple sclerosis, muscle-relaxing Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors. It acts at spinal and supraspinal sites, reducing excitatory transmission.

Riboflavin Tetrabutyrate, a lipophilic flavin derivative, possesses antioxidative and lipid peroxide-removing activities.

Clioquinol (Iodochlorhydroxyquin) is an orally bioavailable, lipophilic, copper-binding, halogenated 8-hydroxyquinoline with antifungal, antiparasitic and potential antitumor activities.

Pantoprazole sodium (Pantecta) is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole sodium is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+ K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.

Revaprazan hydrochloride (YH1885) is the hydrochloride salt form of a lipophilic, weak base with potassium-competitive acid blocking (P-CAB) activity.

Fluticasone furoate (Avamys) is a synthetic trifluorinated corticosteroid derived from fluticasone with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflammatory, anti-asthmatic activity, and low systemic exposure. Fluticasone furoate can be used as a nasal spray for studies about allergic rhinitis treatment.

Pyridinium bisretinoid A2E (A2E) is a fluorescent chromophore isolated from lipofuscin in retinal pigment epithelium, a lipophilic cation and weak photosensitizer with cytotoxicity. A2E promotes apoptosis under blue light exposure and induces autophagy under photoactivation, damaging membrane integrity in a concentration-dependent manner.

Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

Ridaforolimus (AP23573) is a small molecule and non-prodrug analogue of the lipophilic macrolide antibiotic rapamycin with potential antitumor activity. Ridaforolimus binds to and inhibits the mammalian target of rapamycin (mTOR), which may result in cell cycle arrest and, consequently, the inhibition of tumor cell growth and proliferation. Upregulated in some tumors, mTOR is a serine threonine kinase involved in regulating cellular proliferation, motility, and survival that is located downstream of the PI3K Akt signaling pathway.

Brincidofovir (HDP-CDV) is an orally active, lipophilic form of cidofovir. It has enhanced activity compared to CDV against certain adenoviruses, herpesviruses, and orthopoxviruses.

Baclofen hydrochloride (4-amino-3-(4-chlorophenyl)butanoic acid hydron chloride) is a GAMMA-AMINOBUTYRIC ACID derivative that is a specific GABA-B RECEPTORS agonist. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.

Miriplatin hydrate (SM-11355 (hydrate)) (MPT) is a novel platinum complex used in TACE that shows promise for the treatment of hepatocellular carcinoma (HCC). Miriplatin hydrate is a lipophilic platinum complex that can be easily suspended in Lipiodol and gradually releases active platinum compounds in tumor tissue.