PRE-084 hydrochloride

SKU: orb1219602

Description

PRE-084 hydrochloride is a selective agonist of σ1(IC50:44 nM, in the sigma receptor assay).

Key Properties

• CAS Number: 75136-54-8
• MW: 353.88
• Purity: >98% (HPLC)
• Formula: C₁₉H₂₈ClNO₃
• SMILES: Cl.O=C(OCCN1CCOCC1)C1(CCCCC1)c1ccccc1
• Target: Sigma receptor
• Solubility: DMSO:31 mg/mL (87.6mM)

Bioactivity

• In Vivo:
  PRE-084 hydrochloride (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter). PRE-084 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt eNOS pathway in myocardial infarction model. Animal model: Wobbler mice (4-week-old). Dosage: 0.25 mg/kg. Administration: Intraperitoneal injection; 3 times a week for 8 weeks. Result: Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration. Animal model: Adult male Sprague Dawley rats (220-250 g; myocardial infarction model). Dosage: 1 mg/kg. Administration: Intraperitoneal injection; single. Result: Significantly decreased the degree of myocardial apoptosis. Led to significantly increased expression of p Akt and p eNOS.
• In Vitro:
  PRE-084 hydrochloride (0.1-100 μM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 μM) and reduces the levels of proapoptotic protein Bax at 10 μM. Cell Viability Assay Cell line: Cortical cells (βAP(25-35)-induced neurotoxicity model). Concentration: 0.1-100 μM Incubation time: 24 h. Result: Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 μM. Western blot analysis. Cell line: Cortical cells (βAP(25-35)-induced neurotoxicity model). Concentration: 10 μM. Incubation time: 24 h. Result: Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).

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