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saralasin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 3542 | 34273-10-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.303 | High | 0.93 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.637 | High | 0.93 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.333 | 10^-6 cm/s | High | 0.93 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.143 | uL/min/10^6 cells | High | 0.93 |
| dppb | Dog plasma protein binding (% unbound) | 85.140 | % | High | 0.93 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 47.760 | % | High | 0.93 |
| herg | hERG pIC50 | 4.584 | pIC50 | High | 0.93 |
| hh-clint | Human hepatocyte intrinsic clearance | 30.339 | uL/min/10^6 cells | High | 0.93 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.909 | uL/min/mg protein | High | 0.93 |
| hppb | Human plasma protein binding (% unbound) | 74.080 | % | High | 0.93 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK | 18 | |||
| kinase-selectivity-class | GRK2,PDK1 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.113 | High | 0.93 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 36.898 | High | 0.93 | |
| mppb | Mouse plasma protein binding (% unbound) | 62.240 | High | 0.93 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.858 | High | 0.93 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 64.800 | % | High | 0.93 |
| rh-clint | Rat hepatocyte intrinsic clearance | 27.102 | uL/min/10^6 cells | High | 0.93 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 50.580 | % | High | 0.93 |
| rppb | Rat plasma protein binding (% unbound) | 63.210 | % | High | 0.93 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 778.037 | uM | High | 0.93 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA | PROCTER AND GAMBLE |
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 |
|---|---|---|
| MeSH PA | D047228 | Angiotensin II Type 1 Receptor Blockers |
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 | 3.75 | acidic |
| pKa2 | 9.65 | acidic |
| pKa3 | 13.51 | acidic |
| pKa4 | 13.6 | acidic |
| pKa5 | 10.75 | Basic |
| pKa6 | 8.5 | Basic |
| pKa7 | 6.3 | 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 | Ki | 9.77 | CHEMBL | CHEMBL | |||
| Type-2 angiotensin II receptor | GPCR | Ki | 9.82 | CHEMBL | |||||
| Type-1B angiotensin II receptor | GPCR | IC50 | 8.62 | CHEMBL | |||||
| Type-2 angiotensin II receptor | GPCR | ANTAGONIST | IC50 | 9 | IUPHAR | ||||
| Angiotensin II receptor (AT-1) type-1 | GPCR | IC50 | 8.77 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D04126 | KEGG_DRUG |
| 39698-78-7 | SECONDARY_CAS_RN |
| C0036193 | UMLSCUI |
| CHEMBL938 | ChEMBL_ID |
| CHEMBL1200670 | ChEMBL_ID |
| D012504 | MESH_DESCRIPTOR_UI |
| DB06763 | DRUGBANK_ID |
| 598 | IUPHAR_LIGAND_ID |
| 3484 | INN_ID |
| H2AFV2HE66 | UNII |
| 6324663 | PUBCHEM_CID |
| 7830 | RXNORM |
| 000667 | NDDF |
| 004525 | NDDF |
| CHEBI:135894 | CHEBI |
Pharmaceutical products:
None