General
Preferred name
SIRAMESINE
Synonyms
Lu-28-179 ()
Lu 28-179 hydrochloride ()
Siramesine hydrochloride ()
Siramesine (hydrochloride) ()
Lu 28-179 ()
Lu 28-179 (hydrochloride) ()
Siramesine fumarate ()
Siramesine (fumarate) ()
Siramesina ()
P&D ID
PD062151
CAS
224177-60-0
147817-50-3
163630-79-3
Tags
available
drug candidate
Drug Status
investigational
Max Phase
2.0
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
Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3].
PRICE
180
DESCRIPTION
Siramesine is a sigma receptor agonist with selectivity for σ2 over σ1 (IC50 = 0.19 and 17 nM, respectively). It exhibits anxiolytic and antidepressant effects. Siramesine has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
K+/Cl- cotransporter 2 (KCC2) activator; orally bioavailable prodrug of CLP 257 (Cat. No.5242)
(Tocris Bioactive Compound Library)
DESCRIPTION
Siramesine hydrochloride (Lu 28-179 hydrochloride) is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of Y cells and to exhibit a potent anticancer activity in vivo.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
3
Organisms
0
Compound Sets
14
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
DrugMatrix
Mcule NIBR MoA Box Subset
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
38
Molecular Weight
454.24
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
0
Rotatable Bonds
6
Ring Count
6
Aromatic Ring Count
4
cLogP
6.61
TPSA
17.4
Fraction CSP3
0.33
Chiral centers
0.0
Largest ring
6.0
QED
0.3
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Apoptosis
Autophagy
Neuronal Signaling
Target
Ferroptosis
lysosome-destabilizing agent
Sigma Receptor
σ2
ADRA1A, ADRA1B, ADRA1D
Primary Target
?2 Receptors
MOA
Agonist
Sigma receptor antagonist
Member status
member
Source data
