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

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Showing 651 - 660 of 2596 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

JYL1421 is a more selective and in most models a more potent Vanilloid receptor (TRPV1) antagonist than capsazepine, therefore it may promote the assessment of the (patho) physiological roles of the TRPV1 receptor. Vanilloid receptors play a roll in sensory transduction for capsaicin (capsaicin-induced calcium uptake), protons, and heat.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

AL-8810 ((5Z,13E)-(9S,11S,15R)-9,15-Dihydroxy-11- fluoro-15-(2-indanyl)-16,17,18,19,20-pentanor-5,13- prostadienoic acid) is a prostaglandin F2a analog and a selective FP prostanoid receptor antagonist. The mean antagonist potency (Ki) of AL–8810 at the FP prostanoid receptor in both 3T3 fibroblasts and A7r5 vascular smooth muscles cells was 400-500 nM. AL–8810 produced a concentration-dependent shift in the fluprostenol concentration-response curve, without significantly decreasing the maximal response, indicating that AL-8810 is a competitive antagonist. Al-8810 also exhibited similar antagonist potency in inhibiting fluprostenol-stimulated PLC activation in HEK-293 cells expressing the cloned human ocular FP receptor. In contrast, even at 10 mM concentration, AL-8810 did not significantly inhibit DP, EP2, EP4 and IP prostanoid receptors. In a preclinical study, the effect of acute intraperitoneal post-treatment with AL-8810 was studied in FP receptor knockout (FP-/-) mice after controlled cortical impact (CCI). Results showed that post-treatment with AL-8810 had no significant effect on cortical lesions, suggesting the irreversible effect of primary CCI injury, but significantly reduced hippocampal swelling. In addition, AL-8810 treatment at a dose of 10 mg/kg could significantly improve NDS after CCI, and in the AL-8810 group, CCI-induced decrease in grip strength was three-fold less. AL-8810 is a valuable tool for determining specific FP receptor-mediated functions in complex biological systems.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Dimethenamid is a widely used herbicidal compound. It was originally developed by Sandoz Agro and previously marketed as a racemic mixture. It is now known that only the S-isomer exhibits herbicidal activity. The S-isomer is known by the common name dimethenamid-P. Human and animal toxicity are considered low enough for commercial use as a herbicide.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

cis-(-)-Sertraline (aka 1R,4R-sertraline) is the therapeutically inactive enantiomer of Sertraline. Sertraline has four stereoisomers: (1R,4R), (1S,4S), (1R,4S), and (1S,4R), of which the (1S,4S) isomer is the active therapeutic compound. Sertraline is sold under the brand name Zoloft (and others) as an anti-depressant acting as a selective serotonin reuptake inhibitor. The bio-activity of sertraline is restricted to (1S,4S), and (1R,4R), where (1S,4S) is most potent.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Neriifolin is a cardenolide glycoside that is digitoxigenin in which the hydroxy goup at position 3 has been converted to its 6-deoxy-3-O-methyl-alpha-L-glucopyranoside derivative. Found in the seeds of Cerbera odollamand in Thevetia ahouia and Thevitia neriifolia. Neriifolin reduced viability of cancer cells, induced S and G2/M phase arrests of the cell cycle, and stimulated apoptosis.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

A copper fungicide.
α-D-Fucopyranose (aka α-D-fucose) is a six-carbon deoxy monosaccharide. It is equivalent to 6-deoxy-D-galactose. It acts as a non-metabolizable analog of L-arabinose and inhibits induction of the L-arabinose operon in some bacteria. Other bacteria possess a mutant araC gene where D-fucose acts as a gratuitous inducer of the L-arabinose operon. D-fucose also acts as an activator of the galS promotor in E. coli. Because of its ability to regulate gene expression, there has been some interest in exploring D-fucose as a lead compound in neurodegenerative diseases or cancer.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Diethanolamine oleate is clear golden-brown viscous liquid, that used as a surfactant and a corrosion inhibitor. Diethanolamine oleate prolonged mean survival time of mice with Ehrlich exudative carcinoma. The increase in mean survival time after administration of diethanolamine oleate was 8.3%.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gitogenin was first extracted from the herbs of Agave Americana. This compound was found to be a selective inhibitor of UDP- glucuronosyltransferase 1A4 and α-glucosidase, and does not exhibit any inhibition of the major human CYP isoforms. In vitro experiments revealed that gitogenin moderated stimulation for the release of growth hormone from rat pituitary cells.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Cobaltous caprate is an indirect additive used in food contact substances (a component of coatings).