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

Stem definitionDrug idCAS RN
sodium glucose co-transporter inhibitors, phlorizin derivatives 4892 903565-83-3

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tofogliflozin
  • tofogliflozin hydrate
  • deberza
  • apleway
  • CSG452
inhibits sodium-glucose cotransporter 2
  • Molecular weight: 386.44
  • Formula: C22H26O6
  • CLOGP: 3.06
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 99.38
  • ALOGS: -3.07
  • ROTB: 4

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.63 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.07 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.46 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 4.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
March 24, 2014 PMDA

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
MeSH PA D007004 Hypoglycemic Agents
MeSH PA D000077203 Sodium-Glucose Transporter 2 Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diabetes mellitus type 2 indication 44054006 DOID:9352

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.04 acidic
pKa2 12.63 acidic
pKa3 13.27 acidic
pKa4 13.54 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
Sodium/glucose cotransporter 2 Transporter INHIBITOR IC50 8.54 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Sodium/glucose cotransporter 1 Transporter IC50 5.07 SCIENTIFIC LITERATURE

External reference:

IDSource
D09978 KEGG_DRUG
1201913-82-7 SECONDARY_CAS_RN
C4045513 UMLSCUI
CHEBI:136041 CHEBI
RT2 PDB_CHEM_ID
CHEMBL2105711 ChEMBL_ID
CHEMBL2110731 ChEMBL_ID
46908929 PUBCHEM_CID
C575086 MESH_SUPPLEMENTAL_RECORD_UI
DB11824 DRUGBANK_ID
P8DD8KX4O4 UNII
9395 IUPHAR_LIGAND_ID

Pharmaceutical products:

None