Lu-28-179

SKU: orb1225611

Description

Siramesine(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.

Key Properties

• CAS Number: 224177-60-0
• MW: 491.04
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₂ClFN₂O
• SMILES: Cl.FC1=CC=C(C=C1)N1C=C(CCCCN2CCC3(CC2)OCC2=CC=CC=C32)C2=CC=CC=C12
• Target: Sigma receptor
• Solubility: DMSO: 10 mM

Bioactivity

• In Vitro:
  Siramesine hydrochloride displays the binding affinities: IC50 (sigma 1)=17 nM, IC50 (sigma 2)=0.12 nM, IC50 (5-HT1A)=21000 nM, IC50 (5-HT1A)=2000 nM, IC50 (D2)=800 nM, IC50 (alpha 1)=330 nM. Siramesine (0-50 μM; 8 hours) hydrochloride induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG). Siramesine (0-40 μM; 2-48 hours) hydrochloride activates caspases in HaCaT and in U-87MG cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Sigma receptor