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ipragliflozin 🐶 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 | 4890 | 761423-87-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.331 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 6.761 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 22.029 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.623 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 4.840 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 8.390 | % | High | 1 |
| herg | hERG pIC50 | 4.593 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.624 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 5.047 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 4.860 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAP3K21,MAPK10,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PRKDC,TEK,TGFBR1,ZAP70 | 27 | |||
| kinase-selectivity-class | AXL,GRK2,MAP2K6 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 13.092 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 26.424 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 5.770 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 37.844 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 9.560 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 16.672 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 60.110 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 2.770 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 212.324 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 17, 2014 | PMDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Diabetic ketoacidosis | 64.14 | 38.01 | 19 | 627 | 42039 | 110546614 |
| Diabetes mellitus inadequate control | 56.72 | 38.01 | 16 | 630 | 29759 | 110558894 |
| Cerebral infarction | 56.08 | 38.01 | 18 | 628 | 51820 | 110536833 |
| Hypoglycaemia | 45.26 | 38.01 | 19 | 627 | 116085 | 110472568 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A10BK05 | ALIMENTARY TRACT AND METABOLISM DRUGS USED IN DIABETES BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS Sodium-glucose co-transporter 2 (SGLT2) inhibitors |
| MeSH PA | D000077203 | Sodium-Glucose Transporter 2 Inhibitors |
| MeSH PA | D007004 | Hypoglycemic Agents |
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
Related Drugs by ATC class:
A10BK Sodium-glucose co-transporter 2 (SGLT2) inhibitors 7 drugs
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 |
| Diabetes mellitus type 1 | indication | 46635009 | DOID:9744 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.62 | acidic |
| pKa2 | 13.26 | acidic |
| pKa3 | 13.7 | 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 | 8.13 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Sodium/glucose cotransporter 1 | Transporter | IC50 | 5.73 | SCIENTIFIC LITERATURE | |||||
| Sodium/glucose cotransporter 2 | Transporter | INHIBITOR | IC50 | 8.20 | IUPHAR | ||||
| Sodium/glucose cotransporter 1 | Transporter | INHIBITOR | IC50 | 5.86 | IUPHAR | ||||
| Sodium/glucose cotransporter 1 | Transporter | INHIBITOR | IC50 | 5.93 | IUPHAR | ||||
| Sodium/glucose cotransporter 2 | Transporter | INHIBITOR | IC50 | 8.25 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 3N2N8OOR7X | UNII |
| D10196 | KEGG_DRUG |
| 951382-34-6 | SECONDARY_CAS_RN |
| C3492889 | UMLSCUI |
| CHEBI:134724 | CHEBI |
| CHEMBL2018096 | ChEMBL_ID |
| 10453870 | PUBCHEM_CID |
| DB11698 | DRUGBANK_ID |
| CHEMBL4297658 | ChEMBL_ID |
| 9258 | INN_ID |
| C572941 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9394 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
None