General
Preferred name
L-803,087
Synonyms
L-803087 ()
L-803,087 trifluoroacetate ()
P&D ID
PD050579
CAS
217480-26-7
Tags
available
drug candidate
Drug indication
Discovery agent
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
L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice[1][2].
PRICE
452
DESCRIPTION
L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors. L-803087 induces AMPA-mediated synaptic responses in the hippocampus in vitro and increases seizures in alginate-induced seizure-busting mice in vivo.
(TargetMol Bioactive Compound Library)
DESCRIPTION
L-803,087 trifluoroacetate is the trifluoroacetate salt of L-803,087, which is a selective and potent somatostatin sst4 receptor agonist often overexpressed in tumours. Its Ki value is 0.7 nM for cloned human sst4. It is a potential therapeutic target. It can be used to study signaling pathways related to somatostatin receptors. It increases kainate-induced seizures in mice in vivo and facilitates AMPA-mediated hippocampal synaptic responses in vitro.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
11
BOC Sciences Bioactive Compounds
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
DrugMAP
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
18
Molecular Weight
485.22
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
4
Rotatable Bonds
11
Ring Count
3
Aromatic Ring Count
3
cLogP
3.15
TPSA
135.59
Fraction CSP3
0.32
Chiral centers
1.0
Largest ring
6.0
QED
0.14
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
SST1
Somatostatin Receptor
Pathway
GPCR/G protein
Neuronal Signaling
Recommended Cell Concentration
100 nM
Source data
