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Identification
NameNOX-700
Accession NumberDB05464
TypeSmall Molecule
GroupsInvestigational
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.

Structure
Thumb
SynonymsNot Available
External Identifiers Not Available
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
CategoriesNot Available
UNIINot Available
CAS numberNot Available
WeightNot Available
Chemical FormulaNot Available
InChI KeyNot Available
InChINot Available
IUPAC NameNot Available
SMILESNot Available
Taxonomy
ClassificationNot classified
Pharmacology
IndicationInvestigated for use/treatment in diabetes mellitus (type 2).
PharmacodynamicsNOX-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 actionIt 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.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein bindingNot Available
MetabolismNot Available
Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicityNot Available
Affected organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal AbsorptionNot AvailableNot Available
Blood Brain BarrierNot AvailableNot Available
Caco-2 permeableNot AvailableNot Available
P-glycoprotein substrateNot AvailableNot Available
P-glycoprotein inhibitor INot AvailableNot Available
P-glycoprotein inhibitor IINot AvailableNot Available
Renal organic cation transporterNot AvailableNot Available
CYP450 2C9 substrateNot AvailableNot Available
CYP450 2D6 substrateNot AvailableNot Available
CYP450 3A4 substrateNot AvailableNot Available
CYP450 1A2 substrateNot AvailableNot Available
CYP450 2C9 inhibitorNot AvailableNot Available
CYP450 2D6 inhibitorNot AvailableNot Available
CYP450 2C19 inhibitorNot AvailableNot Available
CYP450 3A4 inhibitorNot AvailableNot Available
CYP450 inhibitory promiscuityNot AvailableNot Available
Ames testNot AvailableNot Available
CarcinogenicityNot AvailableNot Available
BiodegradationNot AvailableNot Available
Rat acute toxicityNot AvailableNot applicable
hERG inhibition (predictor I)Not AvailableNot Available
hERG inhibition (predictor II)Not AvailableNot Available
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted PropertiesNot Available
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
References
Synthesis ReferenceNot Available
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
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
Interactions
Drug InteractionsNot Available
Food InteractionsNot Available

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 to many biological processes such as inflammation, immunity, differentiation, cell growth, tumorigenesis and apoptosis. NF-kappa-B is a homo- or heterodimeric complex formed by the Rel-like domain-co...
Gene Name:
NFKB2
Uniprot ID:
Q00653
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 to many biological processes such as inflammation, immunity, differentiation, cell growth, tumorigenesis and apoptosis. NF-kappa-B is a homo- or heterodimeric complex formed by the Rel-like domain-co...
Gene Name:
NFKB1
Uniprot ID:
P19838
Molecular Weight:
105355.175 Da
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Drug created on November 18, 2007 11:25 / Updated on September 13, 2013 12:06