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

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Showing 151 - 160 of 661 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

17α-Epiestriol (17-epiestriol, 16α-hydroxy-17α-estradiol or estra-1,3,5(10)-triene-3,16α,17α-triol) is the 17α-epimer of estriol, a minor hydroxylated estradiol metabolite and a selective estrogen receptor (ER) beta agonist. 17α-Epiestriol is described as a relatively weak estrogen, which is in accordance with its relatively low affinity for the ERα. 17α-Epiestriol has been found to be approximately 400-fold more potent than estradiol in inhibiting tumor necrosis factor α (TNFα)-induced vascular cell adhesion molecule 1 (VCAM-1) expression in vitro.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Conditions:

VcMMAE (valine-citrulline-MMAE) is a drug-linker conjugate for antibody-drug conjugates (ADC) with potent antitumor activity by using the anti-mitotic and cytotoxic drug, monomethyl auristatin E (MMAE). MMAE is linked via the lysosomally cleavable dipeptide, valine-citrulline (vc), which can be specifically hydrolyzed by endosomal proteases, such as cathepsin B. ADCs developed using the valine-citrulline-MMAE (vc-MMAE) platform are studied for the treatment of different types of cancers.
Status:
Other

Class (Stereo):
CHEMICAL (MIXED)


Conditions:

(1,2,6,7-3H)-Testosterone is a radiolabeled form of the corresponding steroid hormone. It can be used to study testosterone metabolism and androgen receptor binding in tissues.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

13-cis Retinol is one of the active metabolite of Vitamin A (all-trans Retinol). 13-cis Retinol is a retinoid inapplicable to the visual processes, and therefore it could be an important catabolic metabolite and its biosynthesis could be part of a process involved in regulating 11-cis-retinol concentrations within the retinal pigment epithelium of 11-cis-retinol dehydrogenase.
Hordenine is a natural Phenethylamine compound that occurs in a number of different plants, but especially barley grass. It is structurally similar to the amino acid Tyramine. It antagonized D2-mediated beta-arrestin recruitment indicating functional selectivity. Hordenine inhibited melanogenesis by suppressing cAMP production, which is involved in the expression of melanogenesis-related proteins. Hordenine may be an effective inhibitor of hyperpigmentation. Hordenine is an indirectly acting adrenergic drug. It liberates norepinephrine from stores. In isolated organs and those structures with reduced epinephrine contents, the hordenine-effect is only very poor. Experiments in intact animals (rats, dogs) show that hordenine has a positive inotropic effect upon the heart, increases systolic and diastolic blood pressure, peripheral blood flow volume, inhibits gut movements but has no effect upon the psychomotorical behavior of mice. Hordenine is considered to be generally very safe and well-tolerated in healthy adults. Hordenine is a nootropic compound that works equally well for cognitive enhancement and athletic performance.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

DL-Cystine is a racemic mixture of the proteinogenic amino acids L-cystine and the non-proteinogenic D-cystine. Cystine is the oxidized dimer form of the amino acid cysteine. L-Cystine serves two biological functions, a site of redox reactions and a mechanical linkage that allows proteins to retain their 3-dimensional structure. DL-cystine is used in the preparation of sulfur-containing dimeric and monomeric surfactants.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Dinitrobenzene (DNB) production yields a mixture of the three isomers. The ortho-isomer (o-DNB) forms colourless to yellow monoclinic plates. o-DNB is a substrate for glutathione-S-aryltransferase. The rapidity of the reaction suggests that this is the main pathway of metabolic o-DNB breakdown in the intact rat liver. o-DNB produced relevant amounts of metHb in human erythrocytes. Dinitrobenzene are used in dyes manufacture, explosives and plastics production.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

(R)-N-(3-(6-(4-(1,4-dimethyl-3-oxopiperazin-2-yl)phenylamino)-4-methyl-5-oxo-4,5-dihydropyrazin-2-yl)-2-methylphenyl)-4,5,6,7-tetrahydrobenzo[b]thiophene-2-carboxamide (GDC-0834) is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). The compound demonstrates effective activity against BCR- and CD40-dependent B-cell proliferation and activation, and potently inhibits immune complex-mediated inflammatory cytokine elaboration in monocytes. In collagen-induced arthritis (CIA) rat models, treatment with oral GDC-0834 demonstrated robust anti-arthritis. GDC-0834 was reported to be extensively metabolized by aldehyde oxidase and carboxylesterase via amide hydrolysis.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Norspermidine (1,7-diamino-4-azaheptane or dipropylenetriamine) is a structural homologue of the natural polyamine spermidine. Norspermidine and its metal complexes exert antineoplastic properties. Dipropylenetriamine NONOate is used as a donor of nitric oxide.

Showing 151 - 160 of 661 results