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saroglitazar 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| dual peroxisome proliferator activated receptors-alpha and gamma(PPAR-alpha,gamma) agonists | 5047 | 495399-09-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a PPARalpha and PPARgamma agonist
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.864 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.416 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 81.470 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 6.808 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.180 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.600 | % | High | 1 |
| herg | hERG pIC50 | 4.727 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 10.023 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 13.062 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.200 | % | High | 1 |
| kinase-safety-class | ACVR2B,AURKA,AXL,BRAF,BTK,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,IKBKB,ITK,MAP2K6,MAPK7,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PRKDC,TGFBR1 | 22 | |||
| kinase-selectivity-class | AXL,GRK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 15.959 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 19.275 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.420 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 38.726 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.510 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 22.131 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 19.930 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.240 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 920.450 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 26, 2013 | CDSCO (INDIA) | CADILA HEALTHCARE |
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 |
|---|---|---|
| CHEBI has role | CHEBI:35526 | hypoglycemic agent |
| CHEBI has role | CHEBI:62868 | hepatoprotective agent |
| CHEBI has role | CHEBI:70782 | PPARα agonist |
| CHEBI has role | CHEBI:71554 | PPARγ agonist |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diabetic dyslipidemia associated with type 2 diabetes mellitus | indication | 761000119102 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 3.58 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor alpha | Nuclear hormone receptor | AGONIST | EC50 | 9.19 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Peroxisome proliferator-activated receptor gamma | Nuclear hormone receptor | AGONIST | EC50 | 8.52 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| E0YMX3S4JD | UNII |
| 1639792-20-3 | SECONDARY_CAS_RN |
| C3852920 | UMLSCUI |
| CHEBI:134708 | CHEBI |
| CHEMBL4297530 | ChEMBL_ID |
| 60151560 | PUBCHEM_CID |
| DB13115 | DRUGBANK_ID |
| 9677 | INN_ID |
| C000588741 | MESH_SUPPLEMENTAL_RECORD_UI |
| 14341 | IUPHAR_LIGAND_ID |
| 1163258006 | SNOMEDCT_US |
| 1172675002 | SNOMEDCT_US |
| EWR | PDB_CHEM_ID |
| E0YMX3S4JD | INXIGHT DRUGS |
Pharmaceutical products:
None