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gamolenic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1276 | 506-26-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An omega-6 fatty acid produced in the body as the delta 6-desaturase metabolite of linoleic acid. It is converted to dihomo-gamma-linolenic acid, a biosynthetic precursor of monoenoic prostaglandins such as PGE1. (From Merck Index, 11th ed)
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.379 | High | 0.96 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.655 | High | 0.96 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 18.923 | 10^-6 cm/s | High | 0.96 |
| dh-clint | Dog hepatocyte intrinsic clearance | 184.502 | uL/min/10^6 cells | High | 0.96 |
| dppb | Dog plasma protein binding (% unbound) | 0.030 | % | High | 0.96 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 0.050 | % | High | 0.96 |
| herg | hERG pIC50 | 4.821 | pIC50 | High | 0.96 |
| hh-clint | Human hepatocyte intrinsic clearance | 758.578 | uL/min/10^6 cells | High | 0.96 |
| hlm-clint | Human liver microsomal intrinsic clearance | 21.086 | uL/min/mg protein | High | 0.96 |
| hppb | Human plasma protein binding (% unbound) | 0.070 | % | High | 0.96 |
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,MAP2K6,MAP3K21,MAP3K7,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIK3CG,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ZAP70 | 54 | |||
| kinase-selectivity-class | AXL,BRAF,EIF2AK3,EPHB4,GRK2,MAP2K6,STK33,TEK | 8 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.410 | High | 0.96 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 264.850 | High | 0.96 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.120 | High | 0.96 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.906 | High | 0.96 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 0.050 | % | High | 0.96 |
| rh-clint | Rat hepatocyte intrinsic clearance | 542.001 | uL/min/10^6 cells | High | 0.96 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 5.900 | % | High | 0.96 |
| rppb | Rat plasma protein binding (% unbound) | 0.050 | % | High | 0.96 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 127.057 | uM | High | 0.96 |
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:
| Source | Code | Description |
|---|---|---|
| ATC | D11AX02 | DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Other dermatologicals |
| ATC | D11AX52 | DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Other dermatologicals |
| CHEBI has role | CHEBI:35842 | antirheumatic drug |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
| CHEBI has role | CHEBI:75771 | mouse metabolite |
| CHEBI has role | CHEBI:76924 | plant metabolite |
| CHEBI has role | CHEBI:77746 | human metabolite |
Related Drugs by ATC class:
D11AX Other dermatologicals 20 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.6 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| 3-oxo-5-alpha-steroid 4-dehydrogenase 2 | Enzyme | IC50 | 4.85 | CHEMBL | |||||
| Peroxisome proliferator-activated receptor alpha | Nuclear hormone receptor | IC50 | 6.57 | CHEMBL | |||||
| Peroxisome proliferator-activated receptor gamma | Nuclear hormone receptor | IC50 | 5.66 | CHEMBL | |||||
| Peroxisome proliferator-activated receptor delta | Nuclear hormone receptor | IC50 | 6.12 | CHEMBL | |||||
| Free fatty acid receptor 1 | GPCR | EC50 | 5.33 | CHEMBL | |||||
| Tissue factor | Membrane receptor | IC50 | 4.52 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| N0000168580 | NUI |
| D07213 | KEGG_DRUG |
| CHEBI:28661 | CHEBI |
| CHEMBL464982 | ChEMBL_ID |
| 2834 | INN_ID |
| DB13854 | DRUGBANK_ID |
| 78YC2MAX4O | UNII |
| 25605 | RXNORM |
| 003969 | NDDF |
| 13121007 | SNOMEDCT_US |
| 427465009 | SNOMEDCT_US |
| C0061078 | UMLSCUI |
| D017965 | MESH_DESCRIPTOR_UI |
| 5280933 | PUBCHEM_CID |
Pharmaceutical products:
None