angiotensin II Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
5272 4474-91-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • angiotensin II
  • giapreza
Angiotensin II is a naturally occurring peptide hormone of the renin-angiotensin-aldosterone system (RAAS) that causes vasoconstriction and an increase in blood pressure. Angiotensin II raises blood pressure by vasoconstriction and increased aldosterone release. Direct action of angiotensin II on the vessel wall is mediated by binding to the G-protein-coupled angiotensin II receptor type 1 on vascular smooth muscle cells, which stimulates Ca2+/calmodulin-dependent phosphorylation of myosin and causes smooth muscle contraction.
  • Molecular weight: 1046.20
  • Formula: C50H71N13O12
  • CLOGP:
  • LIPINSKI: None
  • HAC: 25
  • HDO: 14
  • TPSA: 406.34
  • ALOGS:
  • ROTB: 29

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 23, 2019 EMA La Jolla Pharmaceutical II B.V.
Dec. 21, 2017 FDA LA JOLLA PHARMACEUTICAL CO

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC C01CX09 CARDIOVASCULAR SYSTEM
CARDIAC THERAPY
CARDIAC STIMULANTS EXCL. CARDIAC GLYCOSIDES
Other cardiac stimulants
FDA EPC N0000192562 Vasoconstrictor
FDA PE N0000009908 Vasoconstriction
MeSH PA D002317 Cardiovascular Agents
MeSH PA D014662 Vasoconstrictor Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Septic shock symptomatic treatment 76571007

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.68 acidic
pKa2 3.61 acidic
pKa3 9.65 acidic
pKa4 13.04 acidic
pKa5 13.86 acidic
pKa6 10.75 Basic
pKa7 8.45 Basic
pKa8 6.3 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
Type-1 angiotensin II receptor GPCR AGONIST IC50 9.30 IUPHAR DRUG LABEL
Type-2 angiotensin II receptor GPCR AGONIST Kd 10.20 IUPHAR
Type-1B angiotensin II receptor GPCR Ki 9.51 CHEMBL
Type-1 angiotensin II receptor GPCR Kd 8.24 CHEMBL
Type-1A angiotensin II receptor GPCR IC50 9.40 CHEMBL

External reference:

IDSource
D000804 MESH_DESCRIPTOR_UI
764385008 SNOMEDCT_US
85267009 SNOMEDCT_US
d08691 MMSL
1999003 RXNORM
4037288 VANDF
172198 PUBCHEM_CID
CHEBI:58506 CHEBI
CHEMBL408403 ChEMBL_ID
M089EFU921 UNII
6707 INN_ID
DB11842 DRUGBANK_ID
D00150 KEGG_DRUG
2504 IUPHAR_LIGAND_ID
CHEMBL3989932 ChEMBL_ID
C000627694 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Giapreza HUMAN PRESCRIPTION DRUG LABEL 1 68547-501 INJECTION 2.50 mg INTRAVENOUS NDA 16 sections