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suloctidil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasodilators | 2536 | 54767-75-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A peripheral vasodilator that was formerly used in the management of peripheral and cerebral vascular disorders. It is hepatotoxic and fatalities have occurred. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1312)
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 4.492 | Moderate | 0.68 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 10.351 | Moderate | 0.68 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.652 | 10^-6 cm/s | Moderate | 0.68 |
| dh-clint | Dog hepatocyte intrinsic clearance | 9.333 | uL/min/10^6 cells | Moderate | 0.68 |
| dppb | Dog plasma protein binding (% unbound) | 0.150 | % | Moderate | 0.68 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 1.320 | % | Moderate | 0.68 |
| herg | hERG pIC50 | 5.805 | pIC50 | Moderate | 0.68 |
| hh-clint | Human hepatocyte intrinsic clearance | 41.783 | uL/min/10^6 cells | Moderate | 0.68 |
| hlm-clint | Human liver microsomal intrinsic clearance | 69.663 | uL/min/mg protein | Moderate | 0.68 |
| hppb | Human plasma protein binding (% unbound) | 0.180 | % | Moderate | 0.68 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,IKBKB,ITK,JAK2,JAK3,MAP2K6,MAP3K7,MAPK10,MAPK7,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,ZAP70 | 45 | |||
| kinase-selectivity-class | EIF2AK3,EPHB4,MAP2K6,PDK4 | 4 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.118 | Moderate | 0.68 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 124.738 | Moderate | 0.68 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.240 | Moderate | 0.68 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.358 | Moderate | 0.68 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.840 | % | Moderate | 0.68 |
| rh-clint | Rat hepatocyte intrinsic clearance | 125.314 | uL/min/10^6 cells | Moderate | 0.68 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 0.560 | % | Moderate | 0.68 |
| rppb | Rat plasma protein binding (% unbound) | 0.240 | % | Moderate | 0.68 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 61.518 | uM | Moderate | 0.68 |
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 | C04AX19 | CARDIOVASCULAR SYSTEM PERIPHERAL VASODILATORS PERIPHERAL VASODILATORS Other peripheral vasodilators |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014665 | Vasodilator Agents |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C04AX Other peripheral vasodilators 16 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 | 9.4 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.12 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 7.31 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 6.18 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.86 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.51 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.22 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 6.15 | DRUG MATRIX | |||||
| Histamine H1 receptor | GPCR | Ki | 5.61 | DRUG MATRIX | |||||
| Histamine H2 receptor | GPCR | Ki | 7.05 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 5.97 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 6.01 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.20 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 5.49 | DRUG MATRIX | |||||
| Beta-3 adrenergic receptor | GPCR | Ki | 5.43 | DRUG MATRIX | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.30 | DRUG MATRIX | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.69 | DRUG MATRIX | |||||
| Adenosine receptor A3 | GPCR | Ki | 5.68 | DRUG MATRIX | |||||
| Epidermal growth factor receptor | Kinase | IC50 | 6.10 | DRUG MATRIX | |||||
| Tyrosine-protein kinase Fyn | Kinase | IC50 | 6.14 | DRUG MATRIX | |||||
| Substance-K receptor | GPCR | Ki | 5.65 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 6.26 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D05967 | KEGG_DRUG |
| C0038795 | UMLSCUI |
| CHEBI:233445 | CHEBI |
| CHEMBL404849 | ChEMBL_ID |
| DB13340 | DRUGBANK_ID |
| D013468 | MESH_DESCRIPTOR_UI |
| 6604413 | PUBCHEM_CID |
| 3452 | INN_ID |
| XV1N1XY17K | UNII |
| 004172 | NDDF |
| XV1N1XY17K | INXIGHT DRUGS |
Pharmaceutical products:
None