e-Drug3D

402

DIAZOXIDE


INN
DIAZOXIDE

cas 364-98-7
CLASS

CARDIOVASCULAR
ANTIHYPERTENSIVE
NONDIURETIC BENZOTHIADIAZINE
VASODILATOR AGENTS
MANAGEMENT OF SYMPTOMATIC HYPOGLYCEMIA
INCREASE IN BLOOD GLUCOSE LEVEL SELECTIVE MITOCHONDRIAL KATP-CHANNEL AGONIST
TREATMENT OF HYPERPHAGIA IN PATIENTS WITH PRADER-WILLI SYNDROME (PWS)

ROUTE (list)

INJECTION ORAL

ATC code

C02DA01
V03AH01

PK parameters

Tmax 1 HOUR
VD 13.6 LITER (65 KILOGRAM)
Cl 0.23 LITER / HOUR (65 KILOGRAM)
PPB 94 PERCENT
t1/2 48 HOUR

Solubility

SPARINGLY SOLUBLE IN WATER


Target

TARGET MITOCHONDRIAL KATP-CHANNEL (PMID9400389)

PDB
4LV9 (FRAGMENT-BASED IDENTIFICATION OF AMIDES DERIVED FROM TRANS-2-(PYRIDIN-3-YL)CYCLOPROPANECARBOXYLIC ACID AS POTENT INHIBITORS OF HUMAN NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT))

Ligand code = 20J (link to the list of PDB complexes)

Download experimental 3D coordinates of 20J with added hydrogens

DrugCentral

Sulfonylurea receptor 1, Kir6.2 UNIPROT Q09428 ABCC8_HUMAN

Nicotinamide phosphoribosyltransferase UNIPROT P43490 NAMPT_HUMAN

Download SDF file 7-chloro-3-methyl-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide

Formula:
C8H7ClN2O2S

Calculated chemical properties:

MW 230.68
NB_atoms 14
XLogP 1.87
PSA 58.963
NB_HD 1
NB_HA 4
fsp3 0.12
Lipinski(0=no;1=yes) 1

FDA
NDA 071519 (pdf not found) INN (DIAZOXIDE) DIAZOXIDE (ABRAXIS PHARM) APPROVAL= - YEAR= 0 DISCONTINUED
NDA 071908 (pdf not found) INN (DIAZOXIDE) DIAZOXIDE (QUAD PHARMS) APPROVAL= - YEAR= 0 DISCONTINUED
NDA 016996 (pdf not found) INN (DIAZOXIDE) HYPERSTAT (SCHERING) APPROVAL= AP YEAR= 1973 NEWMOLECULARENTITY DISCONTINUED
NDA 017425 (pdf not found) INN (DIAZOXIDE) PROGLYCEM (TEVA BRANDED PHARM) APPROVAL= AP YEAR= 1976 DISCONTINUED
NDA 017453 (pdf not found) INN (DIAZOXIDE) PROGLYCEM (TEVA BRANDED PHARM) APPROVAL= AP YEAR= 1976
NDA 211050 (pdf not found) INN (DIAZOXIDE) DIAZOXIDE (E5 PHARMA INC) APPROVAL= AP YEAR= 2019
NDA 210799 (pdf not found) INN (DIAZOXIDE) DIAZOXIDE (NOVITIUM PHARMA) APPROVAL= AP YEAR= 2020
NDA 216665 (pdf not found) INN (DIAZOXIDE CHOLINE) VYKAT XR (SOLENO THERAP) APPROVAL= AP YEAR= 2025

Other links:

PubChem
ChemicalProbes

U.S. repository of Clinical Trials

VigiAccess
SIDER side effects

ChemSynthesis
Patent@SureChEMBL