Identification

Name
NOX-700
Accession Number
DB05464
Type
Small Molecule
Groups
Investigational
Description

NOX-700, an new orally active dithiocarbamate-based nitric oxide (NO) blocking agent that is in development for the treatment of diabetes mellitus (type 2 diabetes). In animal studies, NOX-700 lowered serum glucose, improved glucose tolerance, and reduced the percentage of total glycated hemoglobin. Immunohistochemical studies on pancreatic tissue also showed that NOX-700 therapy effectively preserved islet structure and increased insulin immunoreactivity. It has since been found that oxidative signaling of the redox-sensitive transcription factor, NF-κB, and inhibiting protein glycation are responsible for the drug's therapeutic effects.

Synonyms
Not Available
Categories
UNII
Not Available
CAS number
Not Available
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

Investigated for use/treatment in diabetes mellitus (type 2).

Structured Indications
Not Available
Pharmacodynamics

NOX-700 is an orally active nitric oxide (NO) blocking agent in development for the treatment of diabetes mellitus (type 2). In animal studies, NOX-700 lowered serum glucose, improved glucose tolerance, and reduced the percentage of total glycated hemoglobin. Immunohistochemical studies on pancreatic tissue also showed that NOX-700 therapy effectively preserved islet structure and increased insulin immunoreactivity. It has since been found that oxidative signaling of the redox-sensitive transcription factor, NF-κB, and inhibiting protein glycation are responsible for the drug's therapeutic effects.

Mechanism of action

It has been found that oxidative signaling of the redox-sensitive transcription factor, NF-κB, and inhibiting protein glycation are responsible for the drug's therapeutic effects.

TargetActionsOrganism
UNuclear factor NF-kappa-B p100 subunitNot AvailableHuman
UNuclear factor NF-kappa-B p105 subunitNot AvailableHuman
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
Not Available
Food Interactions
Not Available

References

General References
  1. Pieper GM, Khanna AK, Kampalath BN, Felix CC, Hilton G, Johnson CP, Adams MB, Roza AM: Inhibition of nitrosylation, nitration, lymphocyte proliferation, and gene expression in acute and delayed cardiac allograft rejection by an orally active dithiocarbamate. J Cardiovasc Pharmacol. 2004 Apr;43(4):522-30. [PubMed:15085063]
  2. Pieper CM, Roza AM, Henderson JD Jr, Zhu YR, Lai CS: Spatial distribution and temporal onset of NF-kB activation and inducible nitric oxide synthase within pancreatic islets in the pre-diabetic stage of genetic, diabetic-prone BB rats: attenuation by drug intervention decreases inflammatory cell infiltration and incidence of diabetes. Inflamm Res. 2004 Jan;53(1):22-30. Epub 2004 Jan 1. [PubMed:15021977]
  3. Pieper GM, Siebeneich W, Olds CL, Lai CS: Chronic or delayed treatment with an oral dithiocarbamate analog decreases glycation and protects diabetic arteries. Eur J Pharmacol. 2003 Jul 4;472(1-2):127-34. [PubMed:12860481]
External Links
PubChem Substance
347910153

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
Specific Function
NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related...
Gene Name
NFKB2
Uniprot ID
Q00653
Uniprot Name
Nuclear factor NF-kappa-B p100 subunit
Molecular Weight
96748.355 Da
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcriptional repressor activity, rna polymerase ii transcription regulatory region sequence-specific binding
Specific Function
NF-kappa-B is a pleiotropic transcription factor present in almost all cell types and is the endpoint of a series of signal transduction events that are initiated by a vast array of stimuli related...
Gene Name
NFKB1
Uniprot ID
P19838
Uniprot Name
Nuclear factor NF-kappa-B p105 subunit
Molecular Weight
105355.175 Da

Drug created on November 18, 2007 11:25 / Updated on November 06, 2017 06:45