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

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Showing 1921 - 1930 of 21518 results

Status:
Designated
Source:
FDA ORPHAN DRUG:133100
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



3,3',5,5'-Tetraiodothyroacetic acid (Tetrac) is a deaminated analog of L-thyroxine (T4) that blocks the proangiogenesis actions of T4 and 3, 5, 3’-triiodo-L-thyronine as well as other growth factors at the cell surface receptor for thyroid hormone on integrin αvβ3. 3,3',5,5'-Tetraiodothyroacetic acid blocks the transcriptional activities directed by L-thyroxine (T4) and 3,5,3’-triiodo-L-thyronine (T3) at αvβ3, but, independently of T4 and T3, 3,3',5,5'-Tetraiodothyroacetic acid modulates transcription of cancer cell genes that are important to cell survival pathways, control of the cell cycle, angiogenesis (VEGFA, FGF), apoptosis, cell export of chemotherapeutic agents, and repair of double-strand DNA breaks. 3,3',5,5'-Tetraiodothyroacetic acid was found to perturb the angiogenesis process stimulated by VEGF (Vascular Endothelial Growth Factor) or FGF (Fibroblast Growth Factor) without influencing the preexisting blood vessels.
Fenvalerate is type II pyrethroid and widely used pesticide. Fenvalerate is listed under Class IV of the U.S. Food and Drug Administration (USFDA) Surveillance Index Classification, indicating a low hazard potential to humans from both exposure and toxicological standpoints. Fenvalerate irreversibly prolongs the sodium current during depolarization. The sensitization of sodium channels, probably tetrodotoxin-resistant (TTX-R) sodium channels, by the long-term activation of protein kinase C may play an important role in the enhancement of the duration of fenvalerate-induced nociceptive behavior in diabetic mice. Fenvalerate inhibits testosterone synthesis via pathways involving intracellular Ca(2+) and circadian clock genes (Bmal1, Rev-Erb alpha, Ror alpha) as well as StAR mRNA expression in TM3 cells. It potently inhibits human CYP2D6 and moderately CYP3A4. Fenvalerate has an anxiolytic effect on rats.
Status:
Designated
Source:
FDA ORPHAN DRUG:527116
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluasterone is a fluorinated derivative of an endogenous steroid hormone androstenolone (dehydroepiandrosterone, DHEA). According to in vivo studies, fluasterone possess endocrinologic effects manifested in increased estrous cycle length and decreased the weights of the uterus, prostate, seminal vesicles, and testes. The mechanism of action of fluasterone is not yet fully elucidated, but most likely involve inhibition of glucose-6-phosphate hydrogenase. Fluasterone was developed by Aeson Therapeutics and was investigated in the late 1990s for the treatment of asthma, cancer, cardiovascular and metabolic disorders. The development of fluasterone for discontinued, probably due to a combination of low potency and insufficient oral bioavailability. Later, the development of fluasterone was continued by the company SteroTherapeutics. In 2018 the FDA has granted an orphan drug designation for fluasterone for the treatment of nonalcoholic fatty liver disease, nonalcoholic steatosis, and hyperglycemia in patients with Cushing’s syndrome.
Geneticin (G-418) is produced by Micromonospora phodorangea. The antibiotic has brad spectrum antibacterial activity similar to gentamicins and other previously described aminoglycosides but of particular interest because of its high activity against protozoa, amoebae, tapeworm and pinworm infections in mice. G418 blocks polypeptide synthesis by inhibiting the elongation step in both prokaryotic and eukaryotic cells. G418 is commonly used in laboratory research to select genetically engineered cells.
Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:

Showing 1921 - 1930 of 21518 results