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

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Showing 241 - 250 of 2596 results

Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

MDL 201012 is a muscarinic M3 receptor antagonist.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Tetrapotassium Etidronate is the diphosphonic acid derivative. It is used in cosmetics as chelating agent.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

INT is a Tetrazolium derivative, that on reduction produces a red formazan dye that can be used for quantitative redox assays. INT have been used in cytology since the 1950s to detect reducing cell components and later to label metabolically active cells. Also, INT has been adapted in aquatic samples for the in vitro electron transport system (ETS) method, which allows the plankton respiration to be measured with higher sensitivity. INT have been shown to inhibit bacterial growth.
AS-605240 is a potent and selective phosphoinositide 3-kinase (PI3K) gamma inhibitor. It selectively inhibits PI3Kgamma enzymatic activity as well as PI3Kgamma-mediated signaling and chemotaxis in vitro and in vivo. It also has peripheral activity versus other PI3K isoforms. AS-605240 did not progress to clinical development although it had been described as a development candidate.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

ZM 39923 HCl is an JAK1/3 inhibitor with pIC50 of 4.4/7.1 and almost no activity to JAK2 and modestly potent to EGFR. ZM39923 breaks down to form the JAK3 inhibitor ZM449829 which exhibit similar IC50 values. ZM39923 decomposes in neutral buffer to afford potent inhibition of the Janus kinase 3, and could be used as a standard Jak3 inhibitor in assays where breakdown could occur. ZM39923 is reduced by 300-fold in the presence of DTT (10 mM) in inhibiting TGM2. ZM39923 is reversible inhibitors when TGM2 is incubated with inhibitors in the absence of Ca2+. ZM39923 shows significant inhibition of crosslinking activity with IC50 of 25 nM in the absence of DTT and IC50 of 10 μM in the presence of DTT. ZM39923 prevents early death in a Drosophila Melanogaster model of a polyQ repeat disorder called Machado-Joseph Disease. M39923 inhibits the generation of AICD-FLAG and both Aβ40 and Aβ42 by purified γ-secretase in a concentration-dependent fashion with an approximate IC50 of 20 μM. ZM39923 decreases photoaffinity-labeled PS1-CTF in the presense of γ-secretase.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Brassinazole is a synthetic triazole-type inhibitor of the biosynthesis of plant hormones brassinosteroids (BR) that play critical roles in regulating broad aspects of plant growth and development. The structure of brassinazole is similar to pacrobutrazol, a gibberellin biosynthesis inhibitor. Brassinazole has displayed the ability to induce morphological changes in dark-grown Arabidopsis. Additional experiments show that Brassinazole inhibition of plant growth can be prevented by co-application of BR. Brassinazole is a specific inhibitor of C-22 hydroxylase (CYP90B1) in BR biosynthesis, and the application use of brassinazole has emerged as an effective way of complementing BR-deficient mutants to elucidate the functions of BRs.
SR9009 is a research drug that was developed in the laboratory of TSRI Professor Thomas Burris as an agonist of nuclear receptors: Rev-ErbA and Rev-ErbAβ). It was demonstrated that REV-ERBs might be used as a novel target to modulate sleep/wake aberrant behavior.
MS 245 oxalate represents the first member of a novel class of reasonably selective tryptamine-based 5-HT6 receptor antagonists. MS 245 potentiated the hypolocomotor actions, but not the antinociceptive effects, of (-)nicotine in mice. MS 245 together with the ED50 dose of (+)amphetamine resulted in dose-related stimulus generalization. In contrast, the administration of various doses of MS-245 in combination with the ED50 dose of cocaine failed to result in stimulus generalization.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Officinalioside is a new lignan glucoside from Borago officinalis L. Officinalioside showed a moderate DPPH radical scavenging activity (IC50: 41.3 ± 0.25 uM) comparable with that of the standard trolox (16.6 ± 2.2 uM) without any significant cytotoxicity towards human cell line A549 (IC50 > 100 uM).
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

MAM-2201 N-pentanoic acid metabolite is an organic compound that is closely related, structurally, to AM2201 and JWH 122, two compounds which display high affinities for both CB receptors. MAM2201 N-pentanoic acid metabolite is a phase 1 metabolite of JWH-122, but unlike JWH-122, does not show agonistic activity against CB receptors. The physiological and toxicological properties of this compound have not been evaluated.