General
Preferred name
APAFANT
Synonyms
WEB2086 ()
WEB 2086 ()
WEB-2086 ()
DE-081 ()
WEB-2086-BS ()
WEB 2086 BS ()
P&D ID
PD014204
CAS
105219-56-5
Tags
available
free of charge
probe
drug candidate
Drug indication
Ocular allergy
Conjunctivitis
Drug Status
investigational
Max Phase
2.0
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
protein-selective
Probe sources
Chemical Probes.org
High-quality chemical probes
Open Science Probes
opnMe Portal
Probe targets
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 Apafant (WEB 2086 ) is a selective platelet-activating factor (PAF) receptor antagonist.
DESCRIPTION Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, ¦Á-globin, ¦Â-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit[1][2][3].
PRICE 403
DESCRIPTION Apafant (WEB 2086 ) is a selective, water soluble platelet-activating factor (PAF) receptor antagonist. Apafant displays anti-inflammatory, antiangiogenic, and anticancer activity. (GtoPdb)
MOA Antagonist (Chemical Probes.org)
DESCRIPTION Apafant is a potent and specific synthetic antagonist of the pro-inflammatory platelet activating factor (PAF) receptor. In competition experiments with [3H]PAF, Apafant displaces the natural ligand PAF with an equilibrium dissociation constant (KD) of 15 nM, thereby inhibiting the signalling function of PAFR. PAF-induced human platelet and neutrophil aggregation is inhibited in vitro at lC50’s of 170 and 360 nM, respectively. In vivo, extensive investigations using a range of animal models of human disease showed Apafant to potently reduce bronchoconstriction, hypotension, microvascular leakage, and anaphylactic shock amongst many others1,2,3,13. Since its first disclosure in 1987, Apafant has become a widely employed molecule for the in vitro and in vivo study of the PAF pathway, and has been investigated in clinical studies for indications such as asthma4,5. We also provide the PAFR antagonist Bepafant, and its active enantiomer, S-Bepafant. (opnMe Portal)
DESCRIPTION WEB 2086 is a potent and selective platelet-activating factor (PAF) receptor antagonist (Ki = 16.3 nM) potentially used for the treatment of asthma and allergic rhinitis (AR). WEB 2086 exhibits an inhibitory effect on growth and proliferation of MCF-7 breast cancer cells. (BOC Sciences Bioactive Compounds)
DESCRIPTION Potent PAF receptor antagonist (Tocriscreen Plus)
DESCRIPTION Potent PAF receptor antagonist (Tocriscreen Total)
DESCRIPTION Apafant (WEB 2086) is a highly potent platelet activating factor (PAF) antagonist that blocks eosinophil activation and can be used to study experimental allergic conjunctivitis in guinea pigs. (TargetMol Bioactive Compound Library)
DESCRIPTION Selective, high affinity H4 agonist (Tocris Bioactive Compound Library)
Cell lines
0
Organisms
2
Compound Sets
26
BOC Sciences Bioactive Compounds
web-2086-cas-105219-56-5-item-81259
Cayman Chemical Bioactives
14532
ChEMBL Drugs
CHEMBL280164
Chemical Probes.org
apafant
Concise Guide to Pharmacology 2017/18
1860
Concise Guide to Pharmacology 2019/20
1860
Concise Guide to Pharmacology 2021/22
1860
Concise Guide to Pharmacology 2023/24
1860
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DM3AVO1
DrugMatrix
EUbOPEN Chemogenomics Library
EUB0000847
Guide to Pharmacology
1860
1859
High-quality chemical probes
PD014204
Ki Database
WEB2086
MedChem Express Bioactive Compound Library
HY-108634
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Open Science Probes
WEB2086
opnMe Portal
paf-web2086
ReFrame library
TargetMol Bioactive Compound Library
T14300
Tocris Bioactive Compound Library
2339
Tocriscreen Plus
2339
Tocriscreen Total
External IDs
25
Properties
(calculated by RDKit )
Molecular Weight
455.12
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
0
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
3
cLogP
3.43
TPSA
72.61
Fraction CSP3
0.36
Chiral centers
0.0
Largest ring
7.0
QED
0.6
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
7-TM Receptors
Target
PAFR
PTAFR
Platelet activating factor receptor
Platelet-activating Factor Receptor (PAFR)
Primary Target
Platelet-Activating Factor (PAF) Receptors
MOA
Antagonist
PTAFR antagonist
Platelet-Activating Factor Receptor (PAFR) Antagonists
Platelet activating factor receptor antagonist
Member status
member
Pathway
GPCR/G protein
Control name
WEB2387
Target class
GPCR
Target subclass
Platelet-activating factor receptor
Control
BEPAFANT
Recommended Cell Concentration
1 uM
Source data