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Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Conditions:
Acifran (AY-25,712), an uncommercialized Ayerst compound exerting lipid-lowering activity in vivo, has been shown to also elicit similar effects as niacin in preliminary clinical testing and has been shown to bind to both high affinity (HM74A; GPR109A) and low affinity (HM74; GPR109B) niacin receptors. The EC50 values of the separated acifran enantiomers for the GPR109a and 109b receptors showed that, as with acifran itself, the (+)-enantiomers were essentially twice as active as the racemic mixtures, whereas the activity of the (-)-enantiomers was more variable and highly dependent on purity. S-enantiomer of acifran is the active principle. All of the activity of racemic acifran could be attributed to the (S)-enantiomer, and hence, from this precedent, (+)-enantiomers would be assigned to the S-configuration. However, the absolute configuration was not confirmed experimentally.
Status:
Investigational
Source:
NCT03966833: Not Applicable Interventional Completed Mental Depression
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Isopropyl β-D-1-thiogalactopyranoside (IPTG) is a molecular biology reagent that induces β-galactosidase activity in many bacteria. This compound is a molecular mimic of allolactose, a lactose metabolite that triggers transcription of the lac operon, and it is therefore used to induce protein expression where the gene is under the control of the lac operator. Like allolactose, IPTG binds to the lac repressor and releases the tetrameric repressor from the lac operator in an allosteric manner, thereby allowing the transcription of genes in the lac operon, such as the gene coding for beta-galactosidase, a hydrolase enzyme that catalyzes the hydrolysis of β-galactosides into monosaccharides. But unlike allolactose, the sulfur atom creates a chemical bond which is non-hydrolyzable by the cell, preventing the cell from metabolizing or degrading the inducer.
Status:
Investigational
Source:
NCT01530893: Not Applicable Interventional Completed Cardiovascular Disease Risk Reduction
(2012)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Flavanone is the basic chemical skeleton for the class of compounds known as Flavanoids. Flavonoids are naturally occurring secondary plant metabolites. They are mainly found in cereals and herbs. In the western diet, the estimated daily intake of flavonoids is in the range of 20 -50 mg per day. Flavonoids as a class generally have effects on CYP (P450) activity, and therefore may affect drug metabolisms.
Status:
Investigational
Source:
NCT03301454: Phase 2 Interventional Unknown status Esophageal Cancer, Squamous Cell
(2018)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Imazethapyr is an imidazole compound used as a selective herbicide. It is applied preplant incorporated, preemergence, at cracking, and postemergence. The compound controls weeds by reducing the levels of three branched-chain aliphatic amino acids, isoleucine, leucine and valine, through the inhibition of aceto-hydroxyacid synthase, an enzyme common to the biosynthetic pathway for these amino acids. This inhibition causes a disruption in protein synthesis which, in turn, leads to an interference in DNA synthesis and cell growth. The compound is used to control grasses and broadleaved weeds including barnyardgrass, crabgrass, cocklebur, panicums, pigweeds, nightshade, mustard, smartweed, velvetleaf, jimsonweed, foxtails, seedling johnsongrass, lambsquarters, morningglory and others. Tolerant crops include soybeans, peanuts, dry and edible beans, peas, alfalfa and imidazolinone resistant/tolerant corn. Additional research is being conducted on other leguminous crops. Acetolactate synthase inhibition is the primary mechanism of action of imazethapyr (IM).
Status:
Investigational
Source:
NCT01666587: Not Applicable Interventional Completed Ischemic Reperfusion Injury
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(R)-Ibuprofen, a nonsteroidal anti-inflammatory, is the less active enantiomer of ibuprofen. (S)-enantiomer of ibuprofen has the desired therapeutic effect (160 times more active than its (R)-enantiomer) in the in vitro inhibition of prostaglandin synthesis, while the (R)- ibuprofen is inactive. The accumulation of (R)- ibuprofen can cause serious side effects to the human body such as gastrointestinal pain and production of “hybrid” triglycerides between (R)- ibuprofen and Coenzyme A, which disrupt normal lipid metabolism and membrane function. The R(-)-isomer is almost inactive in inhibiting COX-2.
Status:
Investigational
Source:
NCT03262792: Not Applicable Interventional Completed Knee Osteoarthritis
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Neoandrographolide, one of the principal diterpene lactones, isolated from a medicinal herb Andrographis paniculata Nees. Andrographis paniculata (Burm. f.) Wall. ex Nees (Acanthaceae), also known as “kalmegh” in India, is a widely distributed plant in Asia. In many traditional formulations, the aerial parts have been used as anti-inflammatory and antipyretic drugs for the treatment of a variety of chronic and infectious diseases. Neoandrographolide possesses significant anti-inflammatory effects, which implies that it would be one of the major contributing components to participate in the anti-inflammatory effect of A. paniculata. and a potential candidate for further clinical trial.
Status:
Investigational
Source:
NCT03452488: Phase 2 Interventional Completed Sarcopenia
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
20-Hydroxyecdysone is a naturally occurring ecdysteroid hormone, which is marketed as dietary supplements that can increase strength and muscle mass during resistance training, particularly bodybuilding. It was found, that 20-hydroxyecdysone did not affect body composition or training adaptations nor did they influence the anabolic/catabolic hormone status or general markers of catabolism in resistance-trained males. Because is known, that ecdysteroids have been shown to prevent various changes in mammalian tissues after female sex hormone deprivation. 20-Hydroxyecdysone also was investigated on these properties. It was found in rats, that 20-Hydroxyecdysone had a beneficial effect on reducing blood pressure and consequently preventing dilated cardiac hypertrophy. Some in vitro experiments showed, that 20-hydroxyecdysone had effects on lymphocytes and neutrophils, and may act as an immunomodulator.
Status:
Investigational
Source:
NCT03020745: Phase 2 Human clinical trial Completed N/A
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Galactosamine is a hexosamine derived from galactose with the molecular formula C6H13NO5. A few amino sugars, including galactosamine, have been shown to kill tumors in the laboratory. It is unlikely to be used in cancer therapy, however. D-galactosamine is a hepatotoxic, or liver-damaging, agent. Researchers studying animal models of liver failure sometimes use D-galactosamine to induce liver damage. Galactosamine is also helpful for researchers studying agents that might protect the liver from damage.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
(+)-selfotel ((+)-CGS-19755) is an enantiomer of selfotel, a competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptors. The inhibition of NMDA-evoked ACh release from rat striatal slices is stereospecific, with the (+)-enantiomer less potent than the (-)-enantiomer.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Nutlins are cis-imidazoline analogs which inhibit the interaction between mdm2 and tumour suppressor p53. Inhibiting the interaction between mdm2 and p53 stabilizes p53, and is thought to selectively induce a growth-inhibiting state called senescence in cancer cells. These compounds are therefore thought to work best on tumors that contain normal or "wild-type" p53. Nutlin-3 does not induce the phosphorylation of p53 on key serine residues and reveals no difference in their sequence-specific DNA binding and ability to transactivate p53 target genes compared with phosphorylated p53 induced by the genotoxic drugs doxorubicin and etoposide, demonstrating that phosphorylation of p53 on key serines is dispensable for transcriptional activation and apoptosis.