General
Preferred name
SIVELESTAT
Synonyms
ONO-5046.NA ()
Sivelestat sodium salt ()
EI546 sodium tetrahydrate ()
LY544349 sodium tetrahydrate ()
ONO5046 sodium tetrahydrate ()
SIVELESTAT SODIUM ()
ONO5046 sodium ()
EI 546 sodium ()
EI546 sodium ()
ONO 5046 sodium ()
LY-544349 sodium ()
LY544349 sodium ()
ONO-5046 sodium tetrahydrate ()
Elaspol ()
ONO 5046 ()
Elaspol sodium tetrahydrate ()
ONO-5046 ()
Sivelestat sodium hydrate ()
ONO5046 ()
EI546 ()
LY544349 ()
Sivelestat (sodium) ()
Sivelestat (sodium tetrahydrate) ()
ONO5046-Na ()
Sodium sivelestat ()
EI546 (sodium tetrahydrate) ()
LY544349 (sodium tetrahydrate) ()
ONO5046 (sodium tetrahydrate) ()
Sivelestat sodium, ONO5046-Na, Sodium sivelestat, EI546 sodium, LY544349 sodium ()
ONO5046, LY544349, EI546 ()
Sivelestat sodium tetrahydrate ()
Sivelestat (ONO-5046) ()
Sivelestat (sodium salt hydrate) ()
Sivelestat sodium salt tetrahydrate ()
EI-546 ()
LY-544349 SODIUM HYDRATE ()
ONO-5046 SODIUM HYDRATE ()
LY544349 SODIUM HYDRATE ()
LY-544349 ()
P&D ID
PD014273
CAS
150374-95-1
201677-61-4
127373-66-4
Tags
available
drug
drug candidate
Approved by
PMDA
Drug indication
Anterior uveitis
Axial spondyloarthritis
Pyoderma gangrenosum
Rheumatoid arthritis
Crohn disease
Multiple sclerosis
severe acute respiratory syndrome
Psoriatic arthritis
Community-acquired pneumonia
Acute lung injury
Heart disease
Ulcerative colitis
Drug Status
investigational
approved
Max Phase
3.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19[1][2][3][4].
DESCRIPTION Some data is linked to salt forms eg sodium tetra hydrate (PubChem CID 23663985). (GtoPdb)
DESCRIPTION Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19[1][2][3][4].
PRICE 56
DESCRIPTION Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19[1][2][3][4].
PRICE 90
PRICE 41
DESCRIPTION Sivelestat is a competitive human neutrophil elastase (HNE) inhibitor (IC50 = 44 nM, Ki = 0.2 μM). It also inhibits leukocyte elastase obtained from rabbit, rat, hamster and mouse (IC50 = 19 to 49 nM). However, it does not inhibit trypsin, thrombin, plasmin, plasma kallikrein, pancreas kallikrein, chymotrypsin and cathepsin G even at 100 μM. In in-vivo studies, it suppressed lung hemorrhage in hamster (ID50 = 82 μg/kg) by intratracheal administration and increase of skin capillary permeability in guinea pig (ID50 = 9.6 mg/kg) by intravenous administration, both of which were induced by human neutrophil elastase. (BOC Sciences Bioactive Compounds)
DESCRIPTION Sivelestat (ONO5046) is a potent and selective inhibitor of neutrophil elastase with IC50 of 44 nM. (TargetMol Bioactive Compound Library)
DESCRIPTION Pancreatic, gastric and carboxylester lipase inhibitor; antiobesity and antihypercholesterolemic activity (Tocris Bioactive Compound Library)
DESCRIPTION Selective leukocyte elastase inhibitor (Tocriscreen Plus)
DESCRIPTION Sivelestat sodium(ONO5046; LY544349; EI546) is a competitive inhibitor of human neutrophil elastase(IC50 = 44 nM; Ki=200 nM); also inhibited leukocyte elastase obtained from rabbit, rat, hamster and mouse. (BOC Sciences Bioactive Compounds)
DESCRIPTION Sivelestat sodium (EI 546 sodium) is a highly efficient inhibitor of human neutrophil elastase, improving sepsis-induced myocardial dysfunction by activating the PI3K/AKT/mTOR signaling pathway. It can be used in acute lung injury/acute respiratory distress syndrome research. (TargetMol Bioactive Compound Library)
DESCRIPTION Sivelestat sodium tetrahydrate (ONO5046 sodium tetrahydrate) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
26
AdooQ Bioactive Compound Library
A16137
A14073
BOC Sciences Bioactive Compounds
sivelestat-sodium-tetrahydrate-cas-201677-61-4-341319
sivelestat-sodium-cas-150374-95-1-item-84-59388
Cayman Chemical Bioactives
17779
ChEMBL Drugs
CHEMBL3182314
CHEMBL76688
Concise Guide to Pharmacology 2017/18
6441
Concise Guide to Pharmacology 2019/20
6441
Concise Guide to Pharmacology 2021/22
6441
Concise Guide to Pharmacology 2023/24
6441
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12863
DrugCentral
2452
DrugCentral Approved Drugs
2452
DrugMAP
DMOSJD0
DM6BZCV
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
EOS100671
Guide to Pharmacology
6441
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL76688
CHEMBL2107493
MedChem Express Bioactive Compound Library
HY-17443B
HY-17443
HY-17443A
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
ReFrame library
Selleckchem Bioactive Compound Library
sivelestat-sodium
sivelestat-ono-5046
TargetMol Bioactive Compound Library
T6986
T21414
T20762
Tocris Bioactive Compound Library
3535
Tocriscreen Plus
3535
External IDs
74
Properties
(calculated by RDKit )
Molecular Weight
434.11
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
7
Ring Count
2
Aromatic Ring Count
2
cLogP
2.25
TPSA
138.87
Fraction CSP3
0.25
Chiral centers
0.0
Largest ring
6.0
QED
0.45
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
SARS-CoV
Elastase
Neutrophil elastase (human)
Neutrophil Elastase
CELA1, ELANE
Serine Protease
Primary Target
Elastases
MOA
Inhibitor
Leukocyte Elastase Inhibitors
Elastase inhibitor
Member status
member
Indication
acute lung injury
Pathway
Anti-infection
Metabolic Enzyme/Protease
Microbiology/virology
Proteases/Proteasome
Solubility
In vitro:<br/>10 mM in DMSO
Source data