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tofogliflozin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| sodium glucose co-transporter inhibitors, phlorizin derivatives | 4892 | 903565-83-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
inhibits sodium-glucose cotransporter 2
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
| BA (Bioavailability) | 0.98 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2B,BRAF,BTK,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,ZAP70 | 19 | |||
| kinase-selectivity-class | GRK2,MAP2K6 | 2 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 24, 2014 | PMDA |
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:
| Source | Code | Description |
|---|---|---|
| MeSH PA | D000077203 | Sodium-Glucose Transporter 2 Inhibitors |
| MeSH PA | D007004 | Hypoglycemic Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetes mellitus type 2 | indication | 44054006 | DOID:9352 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium/glucose cotransporter 2 | Transporter | INHIBITOR | IC50 | 8.54 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Sodium/glucose cotransporter 1 | Transporter | IC50 | 5.07 | SCIENTIFIC LITERATURE | |||||
| Sodium/glucose cotransporter 2 | Transporter | Ki | 7.83 | CHEMBL | |||||
| Sodium/glucose cotransporter 2 | Transporter | Ki | 8.19 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| P8DD8KX4O4 | UNII |
| D09978 | KEGG_DRUG |
| C3501434 | UMLSCUI |
| RT2 | PDB_CHEM_ID |
| CHEMBL2105711 | ChEMBL_ID |
| 46908929 | PUBCHEM_CID |
| DB11824 | DRUGBANK_ID |
| CHEMBL2110731 | ChEMBL_ID |
| C575086 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9395 | IUPHAR_LIGAND_ID |
| CHEBI:136041 | CHEBI |
| 1201913-82-7 | SECONDARY_CAS_RN |
Pharmaceutical products:
None