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tasosartan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| angiotensin II receptor antagonists, antihypertensive (non-peptidic) | 3839 | 145733-36-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
angiotensin II antagonist; structure given in first source
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| BA (Bioavailability) | 50 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 0.03 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.008 | Moderate | 0.75 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 12.972 | Moderate | 0.75 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 4.613 | 10^-6 cm/s | Moderate | 0.75 |
| dh-clint | Dog hepatocyte intrinsic clearance | 5.105 | uL/min/10^6 cells | Moderate | 0.75 |
| dppb | Dog plasma protein binding (% unbound) | 4.580 | % | Moderate | 0.75 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 8.240 | % | Moderate | 0.75 |
| herg | hERG pIC50 | 4.194 | pIC50 | Moderate | 0.75 |
| hh-clint | Human hepatocyte intrinsic clearance | 15.631 | uL/min/10^6 cells | Moderate | 0.75 |
| hlm-clint | Human liver microsomal intrinsic clearance | 20.941 | uL/min/mg protein | Moderate | 0.75 |
| hppb | Human plasma protein binding (% unbound) | 2.650 | % | Moderate | 0.75 |
| kinase-safety-class | ACVR2B,AXL,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK4,PRKDC | 14 | |||
| kinase-selectivity-class | EIF2AK3 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.904 | Moderate | 0.75 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 29.512 | Moderate | 0.75 | |
| mppb | Mouse plasma protein binding (% unbound) | 4.150 | Moderate | 0.75 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.217 | Moderate | 0.75 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 4.600 | % | Moderate | 0.75 |
| rh-clint | Rat hepatocyte intrinsic clearance | 15.885 | uL/min/10^6 cells | Moderate | 0.75 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 73.590 | % | Moderate | 0.75 |
| rppb | Rat plasma protein binding (% unbound) | 1.620 | % | Moderate | 0.75 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 995.405 | uM | Moderate | 0.75 |
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 | C09CA05 | CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ANGIOTENSIN II RECEPTOR BLOCKERS (ARBs), PLAIN Angiotensin II receptor blockers (ARBs), plain |
| MeSH PA | D047228 | Angiotensin II Type 1 Receptor Blockers |
| MeSH PA | D057911 | Angiotensin Receptor Antagonists |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
Related Drugs by ATC class:
C09CA Angiotensin II receptor blockers (ARBs), plain 9 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.25 | acidic |
| pKa2 | 6.55 | Basic |
| pKa3 | 0.35 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Type-1 angiotensin II receptor | GPCR | ANTAGONIST | IC50 | 7.49 | CHEMBL | SCIENTIFIC LITERATURE | |||
| Angiotensin II receptor (AT-1) type-1 | GPCR | IC50 | 8.92 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D06010 | KEGG_DRUG |
| C0662811 | UMLSCUI |
| CHEBI:135666 | CHEBI |
| CHEMBL432162 | ChEMBL_ID |
| DB01349 | DRUGBANK_ID |
| C086167 | MESH_SUPPLEMENTAL_RECORD_UI |
| 60919 | PUBCHEM_CID |
| 6898 | IUPHAR_LIGAND_ID |
| 7334 | INN_ID |
| 48G92V856H | UNII |
| 48G92V856H | INXIGHT DRUGS |
Pharmaceutical products:
None