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

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Showing 2231 - 2240 of 12702 results

Tioxolone is a metalloenzyme carbonic anhydrase I inhibitor, that has been used for psoriasis vulgaris and acne treatment. Tioxolone is reported to possess cytostatic, antipsoriatic, antibacterial and anti-mycotic properties. Tioxolone is also added to some cosmetics (e.g. hair shampoos and skin cleansers), due to claims for its oil-regulating and antibacterial properties.
Alfaxalone is a rapidly acting hydrophobic synthetic neurosteroid. It is indicated for the induction and maintenance of anesthesia and for induction of anesthesia followed by maintenance with an inhalant anesthetic, in cats and dogs. Alfaxalone induces anaesthesia through activity at the gamma amino butyric acid sub-type A receptor (GABAA) present on cells in the Central Nervous System (CNS). Alfaxalone enhances the effects of GABA at the GABAA receptors resulting in opening of channels into the cells and an influx of chloride ions. This causes hyperpolarisation of the cells and inhibition of neural impulse transmission. Alfaxalone can be safely combined with premedicants (xylazine, (dex)medetomidine, acepromazine, midazolam), opioids (morphine, methadone, hydromorphone, butorphanol, nalbuphine, buprenorphine, fentanyl), and NSAIDs. Alfaxalone’s adverse reactions are: hypotension, tachycardia, apnea, hypertension, bradypnea and others.
Status:
Possibly Marketed Outside US
Source:
Zelcom by OASIS TRADING
Source URL:
First approved in 2018

Class (Stereo):
CHEMICAL (ACHIRAL)



Flubendazole is an anthelmintic that is used to treat worm infection in humans. It is available OTC in Europe. Flubendazole is registered and sold in Europe (EMEA) as Fluvermal (Johnson and Johnson, Sante Bea). A 100mg dose of Fluvermal is most commonly proscribed for treating pinwoms (Enterobius vermiculus)). This is followed by a second dose of 100mg 15-21 days later to ensure reinfection is avoided, as flubendazole does not kill pinworm eggs. 100mg taken 3 times a day for 3 days is effective against larger nematodes, but only marginally effective against tapeworms. Flubendazole was validated for its anti-proliferative efficacy in MDA-MB-231 cells. Moreover, Flubendazole induced autophagy and increased ROS production. In silico analysis and experimental validation together demonstrate that Flubendazole can target autophagy-related protein 4B (Atg4B) in MDA-MB-231 cells and induce autophagy, which may shed light on the exploration of this compound as a potential new Atg4B targeted drug for future triple-negative breast cancer (TNBC) therapy.
Status:
Possibly Marketed Outside US
Source:
part343
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity. The coupling of propyphenazone with other widely used acidic NSAIDs such as ketoprofen, ibuprofen, and diclofenac produced mutual prodrugs with synergistic analgesic effects. It was introduced for the treatment of different types of pain and fever and rheumatic disorders. Propyphenazone structurally relates to aminophenazone it has been associated with severe blood dyscrasias.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Class (Stereo):
CHEMICAL (ACHIRAL)

Bilirubin is an orange-yellow pigment made during the normal breakdown of red blood cells. Bilirubin passes through the liver and is excreted out of the body. Occasionally, higher bilirubin levels may indicate an increased rate of destruction of red blood cells (hemolysis). A high level of bilirubin in the blood is called hyperbilirubinemia. High bilirubin levels can cause jaundice. Jaundice makes the skin and the whites of the eyes appear yellow, due to the brown and yellow bilirubin in the blood. Phototherapy for neonatal is one of the treatment methods against hyperbilirubinemia. Light absorption by bilirubin in the skin transforms the native Z,Z-bilirubin to conformational photoisomers Z,E-bilirubin and E,Z-bilirubin and structural photoisomers E,Z-lumirubin and E,E-lumirubin. Formation and excretion of Z,E-bilirubin and E,Z-lumirubin are both important routes of elimination of bilirubin through bile and urine, although the precise contributions of the various photoisomers to the overall elimination of bilirubin are still unknown.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Lanosterol represents the first step in sterol formation and can be converted by lanosterol 14 α-demethylase (CYP51, a member of the cytochrome P450 family), to follicular fluid meiosis activating factor (FF-MAF), a sterol intermediate that has been extensively studied and shown to activate meiosis in gametes. Lanosterol modulates TLR4-mediated innate immune responses in macrophages. Lanosterol accumulation increases membrane fluidity and ROS production, thus potentiating phagocytosis and the ability to kill bacteria. Preliminary studies in dogs and rabbits have shown that lanosterol can prevent and even reverse cataract formation. However, Lanosterol 25 mM solution did not reverse opacification of human age-related cataractous nuclei. Lanosterol induces mitochondrial uncoupling and protects dopaminergic neurons from cell death in a model for Parkinson's disease.

Showing 2231 - 2240 of 12702 results