U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 321 - 330 of 1076 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



N-Acetyl-α-D-glucosamine (alpha-GlcNAc) is a major component of complex carbohydrates, that has been found in N- and O-glycans and glycolipids. Glycosaminoglycans and the glycosylphosphatidylinositol anchor of membrane-bound glycoproteins also contain GlcNAc moieties. GlcNAc is derived from the degradation of glycoconjugates by glycosidases and from nutritional sources. GlcNAc is converted into GlcNAc-6-phosphate by the N-acetylglucosamine kinase. GlcNAc-6-phosphate can enter a catabolic pathway that ultimately leads to the formation of fructose-6-phosphate, or it can enter an anabolic pathway leading to the formation of UDP-GlcNAc.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

PK-11195 is a selective antagonist of the Translocator Protein (TSPO). The C11 radiolabeled isotope of PK-11195 ([11C]-(R)-PK-11195) has been used effectively for diagnostic PET imaging in a number of CNS conditions where imaging of TSPO is informative (the S- enantiomer is not used). Applicable conditions including Schizophrenia, Multiple Sclerosis, and Traumatic Brain Injuries where it has been particularly useful for detection of increased microglial activation. It has also been investigated as means to monitor the role of Toll-Like Receptor-4 (TLR-4) after cerebral ischemia in mice. It should be noted that the unlabeled PK-11195 had been investigated for a number of potential therapeutic uses but did not progress beyond animal and cell models.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

A-286982 was discovered as a potent, allosteric inhibitor of LFA-1/ICAM-1 interaction, it is known, that A-286982 binds to the IDAS (I domain allosteric site of LFA-1). Lymphocyte function-associated antigen-1 (LFA-1) is a member of leukocyte integrins family and involves in T cells binding to antigen presenting cells. Intracellular adhesion molecule-1 (ICAM-1) is a type of intercellular adhesion molecule and plays a pivotal role in cell-cell interactions. LFA-1/ICAM-1 interaction plays an important role in the pathogenesis of inflammatory disease.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

6-ketocholestanol (5 alpha-Cholestan-3 beta-ol-6-one), a compound increases the membrane dipole potential, it was shown that 6-ketocholestanol was incorporated into unilamellar liposomes and was used as a skin pre-treatment. There was a positive effect of 6-ketocholestanol on the sodium-fluorescein diffusion in all skin types.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Nystatin A1 is the one of the first member of important class of a macrocyclic polyene and poly-ol antibiotics isolated from Streptomyces noursei in 1950. Nystatin A1 binds to ergosterol, a major component of the fungal cell membrane. When present in sufficient concentrations, it forms pores in the membrane that lead to K+ leakage, acidification, and death of the fungus. Nystatin A1 is major component of Nystatin an important antifungal antibiotic, which for over half a century has been broadly used in medicine for the treatment of topical fungal infections caused by a broad spectrum of fungal pathogens comprising yeast-like and filamentous species.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)



gamma-sitosterol is a naturally occurring plant steroid isolatable from plants of the genus Lagerstroemia. Gamma-sitosterol is a potent inhibitor of the complement component C1 complex, and it has demonstrated potential as a diabetic treatment in rats. Gamma-sitosterol is a stereoisomer of beta-sitosterol, which sees wide use as an over the counter natural supplement. However, plant extracts containing gamma-sitosterol have demonstrated toxicity on in-vitro human cell assays; which may discourage use as a natural supplement.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

Gene therapy is expected to treat various incurable diseases including viral infections, autoimmune disorders, and cancers. Complexes of cationic liposomes with DNA are promising tools to deliver genetic information into cells for gene therapy and vaccines. Electrostatic interaction is thought to be the major force in lipid–DNA interaction, while lipid-base binding and the stability of cationic lipid–DNA complexes have been the subject of more debate in recent years. 1,2-Dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE) forms heterogeneous liposomes with cationic lipids, which are used as delivery vehicles for therapeutic agents. DOPE is an essential component of cationic liposomes designed to deliver DNA into gliosarcoma and kidney cell lines (gene therapy). The order of stability of lipid–DNA complexation is DOTAP>DDAB>DOPE>Chol. Recently was discovered Lip-DOPE-MPL-GP2 formulation could be a promising vaccine and a therapeutic delivery system against HER2 positive cancers and merited further investigation.