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

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Showing 361 - 370 of 1076 results

Status:
US Previously Marketed
Source:
PRANONE by SCHERING
(1939)
Source URL:
First approved in 1939

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ethisterone is a metabolite of danazol. Ethisterone is a progestogen hormone. The first orally active progestin, Ethisterone (brand names Pranone, Progestoral, Lutocylol, Proluton C), also known as 17α-ethinyltestosterone, pregneninolone, or anhydrohydroxyprogesterone, is a steroidal progestin with androgenic activity which is derived from testosterone and was introduced for medical use in 1939. Ethisterone is indicated for progesterone supplementation or replacement as part of an Assisted Reproductive Technology (ART) treatment for infertile women with progesterone deficiency and for the treatment of secondary amenorrhea. Also used as a female contraceptive.
Status:
US Previously Marketed
Source:
sodium molybdate
(1921)
Source URL:
First marketed in 1921
Source:
sodium molybdate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Molybdic acid refers to hydrated forms of molybdenum trioxide. There is no information related to the biological and pharmacological application of molybdic acid. It is known, that this substance is used as heterogeneous catalysts.
Status:
US Previously Marketed
Source:
GENTIA-JEL APPLICATORS by WESTWOOD
(1961)
Source URL:
First marketed in 1921
Source:
gentian violet
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Gentian violet ((GV) hexamethyl pararosaniline, also known as crystal violet, methyl violet) is a triphenylmethane dye with anti-bacterial, anti-fungal, anti-helminithic, anti-trypanosomal, anti-angiogenic and anti-tumor properties. GV has a lengthy history and has been used successfully as monotherapy and an adjunct to treatment in a variety of diseases. Gentian violet interacts with negatively charged components of bacterial cells including the lipopolysaccharide (on the cell wall), the peptidoglycan and DNA. A similar cell penetration and DNA binding process is thought to take place for fungal cells as well. Because Gentian violet is a mutagen and mitotic poison, cell growth is consequently inhibited. A photodynamic action of gentian violet, apparently mediated by a free-radical mechanism, has recently been described in bacteria and in the protozoan T. cruzi. Evidence also suggests that gentian violet dissipates the bacterial (and mitochondrial) membrane potential by inducing permeability. This is followed by respiratory inhibition. This anti-mitochondrial activity might explain gentian violet's efficacy towards both bacteria and yeast with relatively mild effects on mammalian cells.
Status:
US Previously Marketed
Source:
cobalamin
(1921)
Source URL:
First marketed in 1921
Source:
cobalamin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cobalamin (vitamin B12) is a cobalt-containing, B complex vitamin. B12 group (cobalamins) consist of cyanocobalamin, hydroxocobalamin, methylcobalamin and cobalamid. Neither plants nor animals are independently capable of constructing vitamin B12. Only bacteria and archaea have the enzymes required for its biosynthesis. Therefore, humans must absorb it from food. Excellent sources of B12 are foods of ruminant origin, so dairy and meat products play an important role in efforts to meet the official daily B12 intake. Vitamin B12 deficiency can potentially cause severe and irreversible damage, especially to the brain and nervous system. Vitamin B12 is used to treat vitamin B12 deficiency, including pernicious anemia.
Status:
US Previously Marketed
Source:
Benzosulphinide U.S.P.
(1921)
Source URL:
First marketed in 1921
Source:
Benzosulphinide U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Saccharin is the most established of the artificial sweeteners on the market, this mixture of dextrose and saccharin has been in use for over a century and is found in diet versions of soft drinks. It is 300-500 times sweeter than sugar and contains zero calories. In 1977, the FDA tried to ban its use after evidence showed it caused cancer in rats. Extensive lobbying by the diet food industry allowed products to stay on the shelves as long as they carried warnings about the cancer risks in animals. This warning was removed in 2001 when the Calorie Control Council insisted the link between animal and human cancers could not automatically be made. Consumption of saccharin-sweetened products can benefit diabetics as the substance goes directly through the human digestive system without being digested. While saccharin has no food energy, it can trigger the release of insulin in humans due to its sweet taste. The T1R2/R3 sweet taste receptor exist on the surface of pancreatic beta cells. Saccharin is a unique in that it inhibits glucose-stimulated insulin secretion (GSIS) at submaximal and maximal glucose concentrations, with the other sweeteners having no effect. Investigation of saccharin’s dose-response characteristics showed that concentrations of 0.1 and 0.5 mM stimulated insulin secretion, while concentrations of 1 and 2.5 mM inhibited insulin secretion. Saccharin’s effect on insulin secretion was shown to be reversible in INS-1 832/13 clonal pancreatic beta cells after chronic exposure to 1 mM saccharin. Artificial sweeteners may affect insulin secretion via interaction with the sweet taste receptor, also saccharin may affect other cellular processes linked to insulin secretion, and that these effects are both time- and concentration-dependent
Proflavine is an acriflavine derivative used as a topical disinfectant agains gram-positive bacteria. Proflavine is toxic and carcinogenic in mammals and so it is used only as a surface disinfectant or for treating superficial wounds. Proflavine acts by interchelating DNA (intercalation), thereby disrupting DNA synthesis and leading to high levels of mutation in the copied DNA strands. This prevents bacterial reproduction. Proflavine was investigated for photodynamic theraphy of herpes but was discontinued due to several presentations of post-treatment Bowen's disease and higher lesion recrudescence periods. Proflavine is also investigated as a topical contrast agent for imaging and diagnosis of esophageal, oral, colon, cervical, uterine cancer and polyps.
Status:
US Previously Marketed
Source:
Veronal by Friedr. Bayer 8: Co., Elberfeld, Germany, and E. Merck, Darmstadt, Germany.
(1903)
Source URL:
First marketed in 1903
Source:
Veronal by Friedr. Bayer 8: Co., Elberfeld, Germany, and E. Merck, Darmstadt, Germany.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Barbital, the one of the series of barbiturates, has hypnotic, sedative, and anticonvulsant properties and used under the trade name Veronal. It calmed manic patients and helped melancholic patients to sleep and was an effective inducer of sleep in insomniacs, but at the same time compound could induced dependence. It was substituted by the butyl analog, butobarbital, which was three times stronger and its period of action was much shorter due to its lipophilicity. Barbital is a ligand of GABA-receptor complex and in addition, it could have another target, a creatine kinase.
Status:
US Previously Marketed
Source:
64 FR 27682 sunscreen 2-ethylhexyl-4-phenylbenzophenone-2-carboxylic acid
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

2-Ethylhexyl-4-phenyl-benzophenone carbonate (Eusolex 3573) is a component of sunscreen and possesses of ultraviolet A (UV-A) absorbing properties.
Status:
Possibly Marketed Outside US
First approved in 2024
Source:
3RX Minoxidil HAIR REGROWTH TREATMENT FOR MEN by Shenzhen Youbente E-commerce Co., Ltd
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Conditions:

Dictamnine, a furoquinoline alkaloid isolated from the root bark of Dictamnus dasycarpus Turcz. (Rutaceae) is reported to have a wide range of pharmacological activities. Dictamnine is a strong mutagen and phototoxic alkaloid with DNA as a cellular target.

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Dibenzoylmethane (DBM), a minor ingredient in licorice, is a calcium chelator that binds calcium through the β-diketone moiety, and it has been found to increase intracellular calcium concentrations in skeletal muscle cells. Intracellular calcium regulates the binding of Nrf2 to the HO-1 enhancer region. Both Nrf2 and HO-1 have been proposed as potential drug targets to prevent or treat liver disease. Thus was suggested DBM could be a lead/candidate for prevention or treatment of liver diseases. In addition, was found, that dibenzoylmethane inhibits mammary tumorigenesis, lymphomas, and leukemias in mice and it can prevent the formation of tumor-inducing DNA adducts.