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

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Showing 231 - 240 of 1447 results

SRT1720 is a small-molecule compound, which has the ability of activating the sirtuin subtype SIRT1. It’s not a direct activation. SRT1720 exhibits multiple off-target activities against receptors, enzymes, transporters, and ion channels. SRT1720 affects mitochondrial respiration in a Sirt1- and PGC-1α-dependent manner. SRT1720 has been demonstrated to enhance insulin sensitivity and improve measures of mitochondrial capacity and oxidative metabolism. SRT1720 also significantly inhibits VEGF-dependent multiple myeloma cell migration. SRT1720 is an experimental drug that was studied by Sirtris Pharmaceuticals. At 2013 year, GlaxoSmithKline was closed down Cambridge, MA-based Sirtris Pharmaceuticals.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

(22S,23S)-homobrassinolide (also known as isohomobrassinolide) is a member of the plant-derived polyhydroxylated derivatives of 5α-cholestane family of compounds; known as brassinosteroids. It was shown that isohomobrassinolide selectively activates the PI3K/Akt signaling pathway by increasing Akt phosphorylation in vitro.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

3-Methylcholanthrene a compound, which can activate both aryl hydrocarbon receptor (AhR) and estrogen receptor alpha. It is used to induce fibrosarcomas and skin carcinomas in laboratory animals. The daily exposure to 3-methylcholanthrene induced changes in both gene expression and epigenomic remodeling, which had led to premature ovarian failure.
Isopteropodine is an Uncaria pentacyclic oxindol alkaloid. It is exhibited antibacterial activity against Gram-positive bacteria. The moderate anti-proliferative effect of isopteropodine was demonstrated on the acute lymphoblastic leukaemia cells. Isopteropodine positively modulate the function of rat muscarinic M1 and 5-HT2 receptors expressed in Xenopus oocyte but further studies are necessary to elucidate the exact mechanism by which isopteropodine positively modulates muscarinic M1 and 5-HT2 receptor functions. Isopteropodine blocked the impairment of passive avoidance performance caused by the nicotinic receptor antagonist mecamylamine and the N-methyl-D-aspartate (NMDA) receptor antagonist (+/-)-3-(2-carboxypiperazin-4-yl)- propyl-1-phosphonic acid (CPP) in mouse model. Moreover, it is possible that the glutamatergic systems are implicated in the anti-amnesic effect of isopteropodine.
Protopanaxadiol (PPD, Yuxintine) is an organic compound characterizing a group of ginsenosides. It is a dammarane-type tetracyclic terpene sapogenin found in ginseng (Panax ginseng) and in notoginseng (Panax pseudoginseng). Protopanaxadiol has a wide range of pharmacologic activities, including antiestrogen, anti-inflammatory, antitumor, vasodilating, cardioprotection, and antidepressant effects. The antidepressant effect of oral Protopanaxadiol had been confirmed by several different animal models, such as forced swimming test tail suspension test, and rat olfactory bulbectomy depression models. Protopanaxadiol was found to have much fewer adverse drug reactions than currently-used first-line antidepressants. It is almostdevoid of sedation, sexual dysfunction, weight gain, cardiovascular complications, and anticholinergic effects. Protopanaxadiol was in phase II clinical trials as a novel antidepressant in China.
Lithocholic acid (LCA) is a secondary bile acid that is formed in the intestine by the bacteria and can activate the pregnane X and the vitamin D receptors. In humans, elevated levels of LCA are found in patients suffering from the chronic cholestatic liver disease. Whereas in normal colonic epithelium lithocholic acid promotes apoptosis, it has been shown to possess anti-tumor effect in human neuroblastoma cell lines. In addition, was proposed, that LCA could kill cancer cells and increase the longevity of non-cancerous cells by causing quite opposite effects on the same kind of mitochondria-confined processes in these two different cell types.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)