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

Stem definitionDrug idCAS RN
prostaglandin receptors antagonists, non-prostanoids 4326 571170-77-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • laropiprant
  • MK 0524
  • MK-0524
a potent orally active human prostaglandin D(2) receptor 1 antagonist
  • Molecular weight: 435.89
  • Formula: C21H19ClFNO4S
  • CLOGP: 3.87
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 1
  • TPSA: 76.37
  • ALOGS: -5.01
  • ROTB: 5

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 1 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.21 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 11.80 hours Lombardo F, Berellini G, Obach RS

Approvals:

None

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:

None

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

DiseaseRelationSNOMED_IDDOID
Dyslipidemia indication 370992007




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 5.04 acidic

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
Prostaglandin D2 receptor GPCR ANTAGONIST Kd 10.52 CHEMBL SCIENTIFIC LITERATURE
Prostaglandin E2 receptor EP1 subtype GPCR Ki 5.94 CHEMBL
Prostaglandin D2 receptor 2 GPCR Ki 6.13 CHEMBL
Prostaglandin E2 receptor EP3 subtype GPCR Ki 6.05 CHEMBL
Prostacyclin receptor GPCR Ki 5.18 CHEMBL
Prostaglandin E2 receptor EP2 subtype GPCR Ki 6.87 CHEMBL
Prostaglandin F2-alpha receptor GPCR Ki 5 CHEMBL
Thromboxane A2 receptor GPCR Ki 8.53 CHEMBL

External reference:

IDSource
D08940 KEGG_DRUG
C1956497 UMLSCUI
CHEBI:135942 CHEBI
CHEMBL426559 ChEMBL_ID
DB11629 DRUGBANK_ID
C518174 MESH_SUPPLEMENTAL_RECORD_UI
3356 IUPHAR_LIGAND_ID
8855 INN_ID
G7N11T8O78 UNII
9867642 PUBCHEM_CID
013266 NDDF

Pharmaceutical products:

None