saralasin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
3542 34273-10-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • saralasin acetate
  • saralasin acetate hydrate
  • saralasin
  • aralasin
An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.
  • Molecular weight: 912.06
  • Formula: C42H65N13O10
  • CLOGP: -5.17
  • LIPINSKI: 3
  • HAC: 23
  • HDO: 13
  • TPSA: 355.05
  • ALOGS: -4.19
  • ROTB: 25

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
None FDA PROCTER AND GAMBLE

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D047228 Angiotensin II Type 1 Receptor Blockers
MeSH PA D057911 Angiotensin Receptor Antagonists

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.75 acidic
pKa2 9.65 acidic
pKa3 13.51 acidic
pKa4 13.6 acidic
pKa5 10.75 Basic
pKa6 8.5 Basic
pKa7 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 ANTAGONIST Ki 9.77 CHEMBL CHEMBL
Type-2 angiotensin II receptor GPCR Ki 9.82 CHEMBL
Type-1B angiotensin II receptor GPCR IC50 8.62 CHEMBL
Type-2 angiotensin II receptor GPCR ANTAGONIST IC50 9 IUPHAR
Angiotensin II receptor (AT-1) type-1 GPCR IC50 8.77 CHEMBL

External reference:

IDSource
D04126 KEGG_DRUG
39698-78-7 SECONDARY_CAS_RN
C0036193 UMLSCUI
CHEBI:135894 CHEBI
CHEMBL938 ChEMBL_ID
CHEMBL1200670 ChEMBL_ID
D012504 MESH_DESCRIPTOR_UI
DB06763 DRUGBANK_ID
598 IUPHAR_LIGAND_ID
3484 INN_ID
H2AFV2HE66 UNII
6324663 PUBCHEM_CID
7830 RXNORM
000667 NDDF
004525 NDDF

Pharmaceutical products:

None