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

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Showing 631 - 640 of 13408 results

Status:
Investigational
Source:
INN:fosmetpantotenate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Phosphopantothenic acid is an amidoalkyl phosphate that is the 4-phosphate derivative of (R)-pantothenic acid. Phosphopantothenic acid is not permeable to cell membranes due to its anionic character, consistent with the observation that systemic administration of Phosphopantothenic acid does not restore CoA levels in cellular and mouse models
Status:
Investigational
Source:
NCT01460420: Phase 1/Phase 2 Interventional Completed Hematologic Malignancies
(2011)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

(±)-quinuclidinyl benzilate (3-quinuclidinyl benzilate), is a specific muscarinic cholinergic receptor antagonist. It binds potently but reversibly to the muscarinic cholinergic receptors of mammalian brain and peripheral tissues. 3-quinuclidinyl benzilate was invented by Hoffmann-La Roche Inc in 1951, while investigating antispasmodic agents resembling tropine for the treatment of gastrointestinal conditions. In the 1960s 3-quinuclidinyl benzilate, was developed and weaponized as a new chemical agent for battlefield use as a psychochemical. Assigned the NATO code BZ it is classified as a hallucinogenic chemical warfare agent that affects both the peripheral and central nervous systems (CNS). It is one of the most potent anticholinergic psychomimetics known, with only small doses necessary to produce incapacitation. The primary route of absorption is through the respiratory system but absorption also can occur through the skin or gastrointestinal tract. BZ is odorless and is usually disseminated as an aerosol. Data regarding the health effects of BZ in humans following inhalation exposure are limited to military application studies. Pharmacologic activity of 3-quinuclidinyl benzilate is similar to other anticholinergic drugs (eg, atropine) but with a much longer duration of action. It was shown that I[3H]-3-quinuclidinyl benzilate accumulated in various brain regions after intravenous injection. The specific binding of [3-3H]3-quinuclidinyl-benzilate and [125I]3-quinuclidinyl-(3-iodo-4-hydroxy-benzilate) to rat brain subcellular fractions is parallel in myelin, synaptic plasma membrane and mitochondrial fractions with a 3-4-fold enrichment observed in synaptic plasma membrane over crude mitochondrial fractions. These findings suggested the use of 3-quinuclidinyl benzilate as a binding probe useful in assaying low levels of muscarinic receptor in tissue culture and other biological sources including labeling the receptor in vivo for autoradiographic studies. M2 muscarinic acetylcholine receptor (M2 receptor), essential for the physiologic control of cardiovascular function through activation of G protein-coupled inwardly-rectifying potassium channels, was shown to bind 3-quinuclidinyl benzilate with high affinity in vitro.
Status:
Investigational
Source:
NCT00095797: Phase 1 Interventional Completed Adult Acute Basophilic Leukemia
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



XK-469 (2-[4-(7-chloro-2-quinoxalinyloxy)phenoxy]-propionic acid) is a novel synthetic quinoxaline phenoxypropionic acid derivative. The R-isomer of XK-469 was approximately twice as effective as the S-isomer of XK-469R. R( )-isomers induce reversible protein DNA crosslinks in mammalian cells. It acts as a selective topoisomerase IIβ inhibitor. A phase I study was performed to determine the safety and pharmacokinetics of XK-469, (R)- in patients with various neoplasms.
Status:
Investigational
Source:
JAN:PARSACLISIB HYDROCHLORIDE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00815763: Phase 3 Interventional Completed Ischemic Stroke
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT01440517: Phase 2 Interventional Terminated Diabetes Mellitus
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Maraciclatide Tc-99m is radiolabelled with technetium 99m cyclic peptide maraciclatide (NC100692 or diamine dioxime-Lys-Cys-Arg-Gly-Asp-Cyc-Phe-Cys-polyethylene glycol). Maraciclatide Tc-99m binds vitronectin receptors (αvβ3 and αvβ5 integrins) with high affinity. Maraciclatide Tc-99m is used in single-photon emission computed tomography (SPECT) imaging of vitronectin receptors that are upregulated and expressed preferentially on proliferating endothelial cells. Maraciclatide Tc-99m is being developed as a diagnostic agent to determine neoplasia and cardiovascular diseases.
Status:
Investigational
Source:
INN:laduviglusib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 for potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.
Status:
Investigational
Source:
NCT03966833: Not Applicable Interventional Completed Mental Depression
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


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:
Clin Nephrol. Feb 1986;25(2):70-4.: Not Applicable Human clinical trial Completed Hyperlipidemias/complications
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pantetheine is the mercaptoethyl conjugated amide analog of pantothenic acid (Vitamin B5), an intermediate in the production of coenzyme A by the body. Pantetheine is part of two larger compounds (coenzyme A and acyl-carrier protein) that promote a large number of metabolic reactions essential for the growth and well-being of animals. Pantetheine has been found to ameliorate symptoms in various disease models but specifically in Pantothenate Kinase-Associated Neurodegeneration (PKAN). Pantetheine is usually administered in its disulfide form (i.e. pantethine) since pantethine is commercially available and is reduced to pantetheine in biological systems and pantethine was hydrolyzed to pantetheine and pantothenic acid prior to absorption. The applicability and efficacy of pantethine (therefore also pantetheine) as a clinical therapeutic however is hampered since both forms can be degraded by pantetheine present in the body.
Status:
Investigational
Source:
NCT01673737: Phase 1 Interventional Completed Neoplasm Malignant
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Sanofi has developed SAR260301 as a selective inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) beta isoform with potential antineoplastic activity. It is known that the dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and contributes to increased tumor cell growth, tumor cell survival. SAR260301 participated in phase I clinical trials in patients with advanced solid tumors. It was found that the drug had an acceptable safety profile, but exposure sufficient to inhibit the PI3K pathway was unachievable because of rapid clearance, and clinical development was terminated.