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Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Azoxystrobin is the first of a new class of pesticidal
compounds called ß-methoxyacrylates, which are derived from the
naturally-occurring strobilurins. Azoxystrobin is a broad spectrum fungicide with activity against several diseases on many edible crops and ornamental plants. Some diseases controlled or prevented are rice blast, rusts, downy mildew, powdery mildew, late blight, apple scab, and Septoria. Azoxystrobin is marketed by Syngenta as single AS products under several trade names, the major ones for crop protection being: Amistar, Abound, Priori, Quadris, Dynasty for seed treatments, and Heritage for turf. Azoxystrobin (AZOX), a Qo inhibitor of mitochondrial respiratory complex III, exerts whole-body beneficial effects on the regulation of glucose and lipid homeostasis in high-fat diet-fed mice. Chronic treatment with AZOX reduced body weight and significantly improved glucose tolerance and insulin sensitivity in high-fat diet-fed mice. AZOX treatment resulted in decreased triacylglycerol accumulation and down-regulated the expression of genes involved in liver lipogenesis. AZOX increased glucose uptake in L6 myotubes and 3T3-L1 adipocytes and inhibited de novo lipogenesis in HepG2 cells.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Asperuloside, an iridoid glycoside found in Herba Paederiae, is a component from traditional Chinese herbal medicine. Asperuloside is extracted from many traditional Chinese medicinal plants, including Herba Paederiae, Asperula odorata, Goldhair Hedyotis Herb and Hedyotis diffusa. It has been proved that there are many kinds of pharmacological effects such as anti-tumor and anti-obesity activities. Asperuloside can significantly downregulate tumor necrosis factor alpha (TNF-α), interleukin (IL)-1β, and IL-6 levels in vitro and in vivo, and treatment with asperuloside significantly reduced the lung wet-to-dry weight, histological alterations and myeloperoxidase activity in a murine model of LPS-induced acute lung injury (ALI). Asperuloside exerts its anti-inflammatory effect in correlation with inhibition of a pro-inflammatory mediator through suppressing nuclear factor kappa-B (NF-κB) nuclear translocation and MAPK phosphorylation. Asperuloside can be a potential treatment for ALI and can be used as a clinical anti-infective drug.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Imetit (S-[2-(4-(imidazolyl)ethyl]isothiourea) is a highly specific and potent histamine H3 receptor agonist. It is widely used to study H3-mediated signaling.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
LG 100268 (LGD 1268) is retionid X receptor agonist, originated in Ligand Pharmaceuticals. LG 100268 demonstrated efficacy in preclinical models of obesity, breast and lung cancer.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Dihydrocholesterol is a cholesterol derivative found in human feces, gallstones, eggs, and other biological matter. Dihydrocholesterol was effective in reducing plasma cholesterol. Plasma total cholesterol-lowering activity of Dihydrocholesterol was mediated by inhibiting the cholesterol absorption and increasing the fecal sterol excretion.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Nomilin is a limonoid/triterpenoid found in citrus fruits that exhibits anti-parasitic, antiviral, anticancer, anti-metastatic, anti-angiogenic, anti-inflammatory, immunomodulatory, anti-obesity, anti-diabetic, and antiviral activities. Nomilin prevents growth of Aedes and suppresses replication of HIV-1 by inhibiting HIV-1 protease. In animal models, nomilin induces phase II enzymes by increasing expression of glutathione-S-transferase and NADPH:Quinone reductase. In animals fed high fat diets, nomilin activates GR5, increases glucose tolerance, and decreases body weight, glucose levels, and insulin levels. In vivo, nomilin increases white blood cell counts and antibody titers but suppresses delayed-type hypersensitivity reactions. In vitro, this compound inhibits cell proliferation, migration, invasion, and capillary tube formation and decreases levels of IL-1β, IL-6, TNF-α, VEGF, NO, and GM-CSF. Additionally, nomilin also inhibits aromatase and cellular proliferation in breast cancer cells. Nomilin also inhibits osteoclastogenesis in vitro by suppression of NFATc1 and MAPK signaling pathways. Nomilin inhibits tumor-specific angiogenesis by downregulating VEGF, NO and proinflammatory cytokine profile and also by inhibiting the activation of MMP-2 and MMP-9.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Omega-hydroxyemodin a naturally occurring anthraquinone derivative isolated from Polygoni cuspidati radix. It has anti-bacterial and phytoestrogen activity. Omega-hydroxyemodin demonstrated topoisomerases I and II inhibition activity. Omega-hydroxyemodin significantly attenuated the DNA binding of activator protein (AP)-1 that regulates COX-2 expression through the reduction of the phosphorylation of c-Jun. Moreover, inhibition of PGD2 generation by Omega-hydroxyemodin was accompanied by a decrease in phosphorylation of cytosolic phospholipase A2α. Taken together, these data suggest that Omega-hydroxyemodin represents a potential therapeutic approach for the treatment of inflammatory diseases. Omega-hydroxyemodin was efficacious in a mouse model of S. aureus skin and soft tissue infections.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Theaflavin is a black tea polyphenol, which possesses a wide variety of pharmacological properties including potent antioxidative, anti-apoptotic, anti-cancer and anti-inflammatory effects. Theaflavin (TF-1) can bind to, and inhibit the purified 20S proteasome, accompanied by suppression of tumour cell proliferation, suggesting that the tumour proteasome is an important target whose inhibition is at least partially responsible for the anticancer effects of black tea. Theaflavin is a potent inhibitor of interleukin-8 gene expression in vitro. The proximal mechanism of this effect involves, in part, inhibition of IkappaB kinase activation and activator protein-1 pathway. Theaflavin has been known to possess neuroprotective effects against ischemia, Alzheimer's disease and other neurodegenerative disorders.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Dehydroabietic acid (also known as NSC18746) is an organic compound that occurs widely in trees. Dehydroabietic acid displays antiulcer, antimicrobial properties and antitumour effects. Dehydroabietic acid has exhibited strong inhibitory effects on EpsteineBarr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
CE-178,253 benzenesulfonate is a CB1 antagonist discovered by Pfizer medicinal chemists. In vitro, CE-178,253 exhibits sub-nanomolar potency at human CB1 receptors in both binding (Ki = 0.33 nM) and functional assays (Ki = 0.07 nM). CE-178,253 has low affinity (Ki > 10,000 nM) for human CB2 receptors. In vivo, CE-178,253 exhibits concentration-dependent anorectic activity in both fast-induced re-feeding and spontaneous nocturnal feeding FI models. In two preclinical models of obesity, CE-178,253 dose-dependently promotes weight loss in diet-induced obese rats and mice.