endralazine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihypertensives, hydrazinephthalazine derivatives 1008 39715-02-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • BQ 22708
  • BQ 22-708
  • endralazine mesilate
  • endralazine mesylate
  • endralazine
  • miretilan
  • Molecular weight: 269.31
  • Formula: C14H15N5O
  • CLOGP: 0.94
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 2
  • TPSA: 84.14
  • ALOGS: -2.68
  • ROTB: 2

Drug dosage:

DoseUnitRoute
10 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 75 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 2.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 13 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 5.60 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C02DB03 CARDIOVASCULAR SYSTEM
ANTIHYPERTENSIVES
ARTERIOLAR SMOOTH MUSCLE, AGENTS ACTING ON
Hydrazinophthalazine derivatives
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.41 Basic
pKa2 4.91 Basic
pKa3 3.77 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel WOMBAT-PK

External reference:

IDSource
D08254 KEGG_DRUG
65322-72-7 SECONDARY_CAS_RN
C0053985 UMLSCUI
CHEBI:135105 CHEBI
CHEMBL254193 ChEMBL_ID
CHEMBL1980706 ChEMBL_ID
DB13435 DRUGBANK_ID
C014926 MESH_SUPPLEMENTAL_RECORD_UI
47608 PUBCHEM_CID
4288 INN_ID
L44741F05P UNII

Pharmaceutical products:

None