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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 271 - 280 of 1447 results

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



Kartogenin is an activator of the smad4/smad5 pathway, and promotes the selective differentiation of multipotent mesenchymal stem cells into chondrocytes. It is promising agent for treatment of osteoarthritis.
Acteoside (verbsacoside) is the one of the main active phenylethanoid glycosides from Cistanche deserticola, Lantana camara and some others herbs. It is known to have antioxidant and neuroprotective activity, and herbs containing it are used to enhance memory and can be studied for the treatment of Alzheimer's disease. It is known, that amyloid fibrils accumulation in cerebral can easily lead to neurodegenerative disorders. Acteoside has been reported to inhibit Aβ42 aggregation by activating nuclear translocation of the transcription factor NF-E2-related factor 2 (Nrf2), increasing heme oxygenase-1 (HO-1) expression. It has also been shown that acteoside could decrease nitric oxide synthase (NOS) activity and caspase-3 expression. Acteoside is a natural antioxidant product unlike other anti-tumor compounds, is an inhibitor of protein kinase C (PKC). In addition Reh-acteoside, a general acteoside of Rehmannia leaves was studied in phase 2/3 clinical trials for patients with IgA nephropathy.
Sophocarpine is a dehydrogenation derivative of the bis-quinolizidine alkaloid matrine. Sophocarpine is also an active component in sophora alkaloids, which possess a variety of pharmacological effects such as anti-inflammation, immunity regulation, antivirus, and anti-tumor actions. Sophocarpine is able to block HERG K+ channel. It is Na+ channel inward current inhibitor. It activates the AMPK signaling pathway and inhibits the TLR4-downstream pathway.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)



BAY-41-2272 is a direct and NO-independent soluble guanylate cyclase (sGC) stimulator. It sensitizes sGC to nitric oxide (NO), its physiological stimulator, and contains antiplatelet activity. BAY-41-2272 is an inhibitor of GCS. BAY-41-2272 inhibits platelet aggregation (IC50 = 36 nM) and phenylephrine-induced contractions of rabbit aorta (IC50 = 0.30 uM). BAY-41-2272 also reduces vascular smooth muscle growth through cAMP- and cGMP-dependent PKA and PKG pathways. BAY-41-2272 not only sensitized NO-sensitive GC toward activation by NO but also, with comparable potency, inhibited cGMP degradation by PDE5. BAY-41-2272 may provide a novel therapeutic compound for treating chronic hypoxic pulmonary hypertension.
Veratridine (VTD), an alkaloid derived from the Liliaceae plant shows anti-tumor effects. Veratridine is also an agent that opens voltage dependent Na+ channels, blocks Na+ channel activation, and induces Ca2+ influx. The compound has been observed to be an alkaloid neurotoxin used to amplify sodium permeability. Studies report that Veratridine can trigger exocytosis and induce Ca2+ oscillations. Furthermore, Veratridine has been shown to effect the mitochondrial respiratory chain complexes, induce release of noradrenaline, and increase superoxide anion production. Veratridine competes with BTX binding in a mutually exclusive manner. However, the pharmacological effects of veratridine on Na+ channels are quite different from those of BTX. First, veratridine reduces the single Na+ channel conductance drastically whereas BTX does not. Veratridine therefore is regarded as a partial agonist and BTX as a full agonist of Na+ channels. Second, under voltage clamp conditions BTX binds practically irreversibly to Na+ channels whereas veratridine readily dissociates from its binding site. Both of these drugs, however, bind preferentially to the open state of Na+ channels. The BTX resistant Na+ channels in Phyllobates frogs remain sensitive to veratridine. The ceveratrum alkaloids, including Veratridine, have a characteristic hypotensive effect not directly involving the CNS. They slow the heart and lower arterial blood pressure by reflexly stimulating medullary vasomotor centers without decreasing cardiac output (Bezold–Jarisch effect). These agents were introduced in the 1950s as antihypertensive agents; however, they were found to have a narrow therapeutic index and their use was discontinued.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

L-Norpseudoephedrine is a psychostimulant drug of amphetamine family, first isolated from an Ephedra species. It is one of the two enantiomers of norpseudoephedrine, less potent that D-Norpseudoephedrine. L-Norpseudoephedrine is a norepinephrine and dopamine releasing agent, and has thermogenic and anorectic effect.
Canthin-6-one is a natural product isolated from various plant genera and from fungi with potential antitumor activity. It induces cell death, cell cycle arrest and differentiation in human myeloid leukemia cells. Canthin-6-one is main compound isolated from Zanthoxylum chiloperone var angustifolium with broad spectrum antifungal, leishmanicidal and trypanocidal activities. Canthin-6-one exhibited trypanocidal activity in vivo in the mouse model of acute or chronic infection. Canthin-6-one exhibited a broad spectrum of activities against Aspergillus fumigatus, A. niger, A. terreus, Candida albicans, C. tropicalis, C. glabrata, Cryptococcus neoformans, Geotrichum candidum, Saccharomyces cerevisiae, Trichosporon beigelii, Trichosporon cutaneum and Trichophyton mentagrophytes var. interdigitale with MICs values between 5.3 and 46 umol/L.