General
Preferred name
reparixin
Synonyms
Repertaxin L-lysine salt ()
DF 1681Y ()
Repertaxin ()
Reparixin (L-lysine salt) ()
Reparixin L-lysine salt ()
Reparixin (Repertaxin) ()
Reparixin (L-Lysine salt) ()
REPARIXINE ()
REPARIXINA ()
DF-1681Y ()
DF1681Y ()
P&D ID
PD012612
CAS
266359-83-5
266359-93-7
Tags
available
drug candidate
Drug indication
Ischemia-reperfusion injury
Pancreatic islet transplantation failure
Graft rejection in heart transplantation
lung transplantation
chronic pancreatitis
Drug Status
investigational
Max Phase
3.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Reparixin L-lysine salt is an allosteric inhibitor of chemokine receptor 1/2 (CXCR1/2) activation.
PRICE
50
DESCRIPTION
Reparixin is an orally bioavailable compound that has been explored for potential to disrupt IL-8/CXCR1/2 signalling in cancer and transplant indications. It negatively modulates CXCR1 and CXCR2 dependent functions , but without inhibiting chemokine binding to either receptor. Direct binding to CXCR1 has only been indicated by molecular modelling, so the mechanism of action of this molecule remains to be fully resolved.
(GtoPdb)
DESCRIPTION
Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
PRICE
132
DESCRIPTION
The efficacy of RPX (tested in a wide range of concentrations (1-1000 nM)) was lower in cells expressing Ile43Val CXCR1 mutant (IC50 values of 0.0056 and 0.08 uM for CXCR1 weight and CXCR1 Ile43Val, respectively). Treatment with reparixin significantly counteracts secondary degeneration by reducing oligodendrocyte apoptosis, migration to the injury site of neutrophils and ED-1-positive cells.
The best beneficial outcome of reparixin treatment required 7-day administration either by i.p. route (15 mg/kg) or subcutaneous infusion via osmotic pumps (10 mg/kg), reaching a steady blood level of 8 microg/ml. Reparixin effectively decreased systolic blood pressure and increased the blood flow. The thoracic aorta wall thickness was significantly decreased in SHR-R compared to SHR-N. Pre-treatment with reparixin reduced the motor deficits observed in this model of ischemia and reperfusion. Myeloperoxidase activity and IL-iβ were reduced in the reparixin-treated group. Histological analysis revealed that ischemic injury was also attenuated by reparixin pre-treatment. (BOC Sciences Bioactive Compounds)
The best beneficial outcome of reparixin treatment required 7-day administration either by i.p. route (15 mg/kg) or subcutaneous infusion via osmotic pumps (10 mg/kg), reaching a steady blood level of 8 microg/ml. Reparixin effectively decreased systolic blood pressure and increased the blood flow. The thoracic aorta wall thickness was significantly decreased in SHR-R compared to SHR-N. Pre-treatment with reparixin reduced the motor deficits observed in this model of ischemia and reperfusion. Myeloperoxidase activity and IL-iβ were reduced in the reparixin-treated group. Histological analysis revealed that ischemic injury was also attenuated by reparixin pre-treatment. (BOC Sciences Bioactive Compounds)
DESCRIPTION
Reparixin L-lysine salt (Repertaxin L-lysine salt) is an allosteric chemokine receptor 1/2 (CXCR1/2) activation inhibitor.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Reparixin (Repertaxin) is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
21
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
Other bioactive compounds
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
40
Molecular Weight
283.12
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
1
Aromatic Ring Count
1
cLogP
2.06
TPSA
63.24
Fraction CSP3
0.5
Chiral centers
1.0
Largest ring
6.0
QED
0.9
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
CXCR
CXCR1
CXCR1Ile43Val
CXCR1wt
CXCR2
CXCR1, CXCR2
MOA
CXCR inhibitor
CC chemokine receptor antagonist
Pathway
Autophagy
GPCR/G protein
Immunology/Inflammation
Recommended Cell Concentration
100 nM
Source data
