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

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Showing 641 - 650 of 1447 results

Thioctic acid amide is a coenzyme, which transfer acetyl and hydrogen in pyruvate deacylation oxidation process, used for pharmaceuticals. Thioctic acid amide has been described as antioxidant, preventing oxidant-mediated apoptosis. It may be used in treatment of insulin resistance by stimulating mitochondrial biogenesis. When used in combination with Alprostadil, it has shown to have a good therapeutic effect on early diabetic nephropathy. Thioctic acid amide is an ingredient of Lipochol, used for prevention of liver diseases, hepatoprotection from drugs, autointoxication.
Solasonine, a known glycoalkaloid, is a potential anti-cancer agent. Solasonine is a component of Curaderm BEC5 indicated for the topical treatment of actinic keratosis, keratoacanthoma, basal cell carcinoma and cutaneous superficial squamous cell carcinoma. BEC is a standardized mixture of Solamargine (33%), Solasonine (33%) and di-and monoglycosides of solasodine (34%) extracted from S. sodomaeum, now reclassified as S. linnaeanum. Solasonine could inhibit cell proliferation, migration and colony formation of glioma cells. Treatment of solasonine induced apoptosis via modulating cytochrome c and caspase signaling. Besides, solasonine decreased the expression of proinflammatory mediators and nuclear translocalization of NF-κB p50/p65. Mechanistic investigation further revealed that solasonine may target anti-inflammatory signaling pathway, and more specifically p-p38 and p-JNK MAPKs.
Status:
Possibly Marketed Outside US
Source:
Parastar® Plus by Sumitomo Chemical
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Cyphenothrin is one of the type II pyrethroid insecticide, in combination with fipronil it used to provide dogs with protection to common topical parasites in dogs. Cyphenothrin primarily affects sodium channels in excitable membranes causing a prolongation of the sodium current during excitation. The prolonged sodium current results in the development of a depolarizing after potential following the action and is responsible for the induction of repetitive activity, which is the most characteristic effect of pyrethroid poisoning in the nervous system. At low concentrations, insects and other arthropods suffer from hyperactivity. At high concentrations, they are paralyzed and die.
Status:
Possibly Marketed Outside US
Source:
GENCOR by Henrick, C.A.
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Hydroprene is a synthetic version of the insect hormone that regulates growth and development. Hydroprene can be considered as an alternative to conventional insecticides because of its specific activity against immature insect stages, low persistence in the environment, and virtually non-toxic effects on mammals. Hydroprene products are used on a variety of indoor sites including homes, offices, warehouses, restaurants, hospitals, and greenhouses.
Status:
Possibly Marketed Outside US
Source:
ZAP AK by Soderlund, D.M.|Casida, J.E.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Cyphenothrin, (+)-trans- (d,d,trans-cyphenothrin) is the type II pyrethroid insecticide, acting by contact poisoning Cyphenothrin, (+)-trans- is used in public health against flies, mosquitoes, cockroaches, etc. Cyphenothrin is the ISO common name for a racemic mixture of 4 pairs of diastereoisomers, designated as (±)-α-cyano-3- phenoxybenzyl (±)-cis-trans- chrysanthemate. The name Cyphenothrin, (+)-trans- refers to an enantio-enriched mixture, comprised mainly of the single stereoisomer (S)-α-cyano-3- phenoxybenzyl (1R, 3R)-2,2-dimethyl-3-(2-methylprop-1-enyl) cyclopropanecarboxylate, with only small proportions of the other stereoisomers, as defined by the WHO specification. Cyphenothrin, (+)-trans- is almost insoluble in water but highly soluble in organic solvents, such as hexane, ethanol, acetone, toluene etc. Cyphenothrin, (+)-trans- stable under normal storage conditions but is readily hydrolyzed in water at higher pH and is sensitive to light. Cyphenothrin, (+)-trans- has a low potential for bioaccumulation due to hydrolysis, photolysis and metabolism in water, soil and in biota. The data for toxicology of Cyphenothrin, (+)-trans- partly rely on studies conducted with cyphenothrin. Cyphenothrin, (+)-trans- generally shows low mammalian toxicity and is not a sensitizer in the Buehler and is not irritating to the rabbit eye and skin. There was no evidence of carcinogenicity in the rat or mouse. There was no evidence of mutagenic responses in bacterial, micronucleus or sister chromatid exchange tests. In a 2-generation reproduction study in the rat, no reproductive effects were observed at any dose level. There was no evidence of teratogenicity or developmental effects in rats or rabbits, although there was a decrease in maternal weight gain and a consequential decrease in rat offspring viability at the high dose tested. Cyphenothrin, (+)-trans- is very toxic to Daphnia magna and fish but it has a low toxicity to bobwhite quails. On the basis of the one-year dog study, a NOEL of 16.8 to 19.6 mg/kg bw/d is established by the Swiss Office of Public Health. The Cyphenothrin, (+)-trans- TC was classified as moderately toxic (Class 3) in Switzerland and, although it has not been classified by the International Programme on Chemical Safety (IPCS), this organization has classified the closely related cyphenothrin (1R-isomers) as Class II, moderately hazardous.
Status:
Possibly Marketed Outside US
Source:
Bicyclol by Chinese Academy of Medical Sciences
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Bicyclol, also known as SY 801, is a hepatoprotective agent. Bicyclol upregulates transcription factor Nrf2, HO-1 expression and protects rat brains against focal ischemia. Bicyclol induces cell cycle arrest and autophagy in HepG2 human hepatocellular carcinoma cells through the PI3K/AKT and Ras/Raf/MEK/ERK pathways. Bicyclol attenuates tetracycline-induced fatty liver associated with inhibition of hepatic ER stress and apoptosis in mice. Bicyclol promotes toll-like 2 receptor recruiting inosine 5'-monophosphate dehydrogenase II to exert its anti-inflammatory effect. Phase Ⅰ~Ⅳ clinical trials and extensive application after market launch prove that, Bicyclol is suitable for the treatment of chronic viral and non-viral liver disease with elevated serum aminotransferase abnormalities, and is excellent in safety. This drug is recommended for liver protection and anti-inflammatory medication by Chinese Medical Association in Guidelines for Management of Alcoholic Fatty Liver Disease, Guidelines for Management of Non-alcoholic Fatty Liver Disease, The Guideline of Prevention and Treatment for Chronic Hepatitis B, Expert Consensus On Hepatic Inflammation and Its Prevention and other professional guidelines and consensus.
Ginsenoside C is a triterpene saponin originally found in species of Panax (ginseng) that exhibits anti-osteoporotic, antioxidative, antiviral, anti-hyperlipidemic, anti-metastatic, anti-angiogenic, and anticancer chemotherapeutic activities. In vivo, ginsenoside C decreases levels of malondialdehyde and increases levels of glutathione, improving bone microarchitecture and bone mineral density. In other animal models, this compound decreases virus titers and protects against infection of hemagglutinating virus of Japan. In adipocytes, ginsenoside C decreases levels of cholesterol and triglycerides and increases expression of SREBP. In uterine endometrial cancer cells, ginsenoside C decrease expression of matrix metalloproteinase 2 (MMP2), suppressive cellular invasion; this compound also inhibits neovascularization and tumor growth in animal models of melanoma. Ginsenoside C is a component of Korean Red Ginseng, marketed in Korea. Korean ginseng (Panax ginseng Meyer, Araliaceae) is traditionally used as an important herbal medicine in Far East Asia. Korean Red Ginseng is possibly effective for: • Alzheimer's disease. Evidence shows that taking Panax ginseng root daily for 12 weeks can improve mental performance in people with Alzheimer's disease. • Lung disease called chronic obstructive pulmonary disease (COPD). Taking Panax ginseng by mouth seems to improve lung function and some symptoms of COPD. • Mental function. Taking Panax ginseng by mouth might improve abstract thinking, mental arithmetic skills, and reaction times in healthy, middle-aged people but not in young adults. Panax ginseng alone does not seem to improve memory. But there is some evidence that a combination of Panax ginseng and ginkgo leaf extract can improve memory in otherwise healthy people between the ages of 38 and 66. • Erectile dysfunction (ED). Taking Panax ginseng by mouth seems to improve sexual function in men with erectile dysfunction. • Flu. Taking a specific Panax ginseng by mouth appears to reduce the risk of getting a cold or the flu. But, taking Panax ginseng does not seem to reduce flu symptoms or the length of the illness. • Multiple sclerosis-related fatigue. Taking Panax ginseng daily for 3 months reduces feelings of tiredness and improves quality of life in females with MS. • Premature ejaculation. Applying a cream containing Panax ginseng, angelica root, Cistanches deserticola, Zanthoxyl species, torlidis seed, clover flower, asiasari root, cinnamon bark, and toad venom (SS Cream) to the penis one hour before intercourse and washing off immediately before intercourse seems to help prevent premature ejaculation.
Kavain is the main kavalactone found mostly in the roots of the kava plant. Kavain interacts with voltage-dependent Na+ and Ca2+ channels, GABAA ion channels. Kavain is found to be involved in TNF-alpha expression in human and mouse cells via regulation transcriptional factors. Kavain exhibits neuroprotective effects in models of Alzheimer's and Parkinson's diseases, and produces anxyolitic effect.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ginsenoside Rb1 is a triterpene saponin originally found in species of Panax that exhibits antioxidative, anti-inflammatory, neuroprotective, orexigenic, and stimulatory activities. In animal models, ginsenoside Rb1 increases motor activity, food intake, and skeletal muscle ATP content, improving energy metabolism. Ginsenoside Rb1 also downregulates expression of toll-like receptor 4 (TLR4) and TNF-α in animal models of sepsis, protecting against liver and lung damage. Additionally, ginsenoside Rb1 inhibits glucose-induced neurotoxicity by preventing GSK-3β-stimulated CHOP induction. This compound also activates Nrf2 and increases expression of heme oxygenase 1 (HO-1), suppressing oxidative stress in vitro. Ginsenoside Rb1 improves learning and memory, increases Bmax of M-cholinergic receptors, and accelerates cerebral protein and ACh biosynthesis. Ginsenoside Rb1 is a component of Korean Red Ginseng, marketed in Korea. Korean ginseng (Panax ginseng Meyer, Araliaceae) is traditionally used as an important herbal medicine in Far East Asia. Korean Red Ginseng is possibly effective for:
Ginsenoside Rg3 (Rg3) is one of the most effective steroidal saponins extracted from Ginseng, a common Traditional Chinese medicine (TCM) herb which tonifies Qi in TCM theory and inhibits tumors. Rg3 suppresses tumor growth and tumor angiogenesis. For its significant antitumor effects, Rg3 has been used in clinical trials in combination with chemotherapy regimens. 20(S) and 20(R) forms of ginsenosides are stereoisomers of each other that depend on the orientation of the C-20 hydroxyl in ginsenosides. In general, the 20(S) compounds have been shown to possess better anti-proliferative effects than their 20(R) counterparts whereas 20(R) compounds such as 20(R)-Rg3 have been shown to inhibit cancer cell invasion and metastasis. Ginsenoside Rg3 regulates voltage-gated ion channels such as Ca(2+), K(+), and Na(+) channels, and ligand-gated ion channels such as GABAA, 5-HT3, nicotinic acetylcholine, and N-methyl-D-aspartate (NMDA) receptors through interactions with various sites including channel blocker binding sites, toxin-binding sites, channel gating regions, and allosteric channel regulator binding sites when the respective ion channels or receptors are stimulated with depolarization or ligand treatment. Shenyi capsule which contains ginsenoside Rg3 as the main ingredient has been approved by China Food and Drug Administration (CFDA) to be used clinically for cancer treatment.