Description
Siramesine is an agonist for sigma-2 (σ2) receptor. It is selective for σ2 over σ1 with IC₅₀ values of 0.12 nM and 17 nM respectively. It shows potent anxiolytic-like effects in rodents. The minimal effective dose (MED) is 0.18 nmol/kg (0.1 microg/kg) and 0.00018 nmol/kg (0.1 ng/kg) in rats and mice respectively. It (20-30 μM) induces cell death in HaCaT, Hsc-4, HeLa, MCF-7, SH-SY5Y and glioblastoma cell lines. Siramesine shows anti-viral activity againt SARS-CoV-2 infection in the Vero E6 cell line in an immunofluorescence-based assay (detecting the viral NP protein).
Siramesine is an agonist for sigma-2 (σ2) receptor. It is selective for σ2 over σ1 with IC₅₀ values of 0.12 nM and 17 nM respectively. It shows potent anxiolytic-like effects in rodents. The minimal effective dose (MED) is 0.18 nmol/kg (0.1 microg/kg) and 0.00018 nmol/kg (0.1 ng/kg) in rats and mice respectively. It (20-30 μM) induces cell death in HaCaT, Hsc-4, HeLa, MCF-7, SH-SY5Y and glioblastoma cell lines. Siramesine shows anti-viral activity againt SARS-CoV-2 infection in the Vero E6 cell line in an immunofluorescence-based assay (detecting the viral NP protein).
Alternate Name/Synonyms: Lu-28-179; 1'-[4-[1-(4-fluorophenyl)indol-3-yl]butyl]spiro[1H-2-benzofuran-3,4'-piperidine]; 1'-(4-(1-(p-Fluorophenyl)indol-3-yl)butyl)spiro(phthalan-1,4'-piperidine)
Appearance: White solid
Formulation:
CAS Number: 147817-50-3
Structure Available?: TRUE
Peptide sequence:
Salt Form: FALSE
Molecular Formula: C₃₀H₃₁FN₂O
Molecular Weight: 454.6
Cell-Permeable?: TRUE
Purity: ≥98%
Solubilities: ~25 mg/ml in DMSO
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: An agonist for sigma-2 receptor
MDL Number: MFCD00912182
PubChem CID: 9829526
SMILES: C1CN(CCC12C3=CC=CC=C3CO2)CCCCC4=CN(C5=CC=CC=C54)C6=CC=C(C=C6)F
InChi: InChI=1S/C30H31FN2O/c31-25-12-14-26(15-13-25)33-21-23(27-9-2-4-11-29(27)33)7-5-6-18-32-19-16-30(17-20-32)28-10-3-1-8-24(28)22-34-30/h1-4,8-15,21H,5-7,16-20,22H2
InChi Key: XWAONOGAGZNUSF-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |