Description
PRE-084 is a high affinity sigma receptor 1 (σ1) agonist. It shows Ki values of 2.2 and 13,091 nM for σ1 and σ2 receptors, respectively and an IC₅₀ of 44 nM in the sigma receptor assay. It does not show significant activity for PCP and other receptors (IC₅₀ > 10,000 nM). PRE-084 has beneficial effects in a cellular model of Huntington's disease. It (0.3 μM) decreases the deleterious effects of N-terminal mutant huntington proteins in neuronal PC6.3 cells by activating NF-κB pathway and decreasing oxidative stress. Modulators of sigma receptor 1 may be beneficial against SARS-CoV-2 based on interaction of sigma receptors with SARS-CoV-2 protein Nsp6.
PRE-084 is a high affinity sigma receptor 1 (σ1) agonist. It shows Ki values of 2.2 and 13,091 nM for σ1 and σ2 receptors, respectively and an IC₅₀ of 44 nM in the sigma receptor assay. It does not show significant activity for PCP and other receptors (IC₅₀ > 10,000 nM). PRE-084 has beneficial effects in a cellular model of Huntington's disease. It (0.3 μM) decreases the deleterious effects of N-terminal mutant huntington proteins in neuronal PC6.3 cells by activating NF-κB pathway and decreasing oxidative stress. Modulators of sigma receptor 1 may be beneficial against SARS-CoV-2 based on interaction of sigma receptors with SARS-CoV-2 protein Nsp6.
B3049 | PRE-084 Hydrochloride DataSheet
Alternate Name/Synonyms: 2-morpholin-4-ylethyl 1-phenylcyclohexane-1-carboxylate;hydrochloride
Appearance: White to Off-White Solid
Formulation:
CAS Number: 75136-54-8
Structure Available?: TRUE
Peptide sequence:
Salt Form: TRUE
Molecular Formula: C₁₉H₂₈ClNO₃
Molecular Weight: 353.88
Cell-Permeable?: TRUE
Purity: ≥98%
Solubilities: ~1.1 mg/ml in DMSO and DMF
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: A high affinity sigma receptor 1 agonist
MDL Number: MFCD00153919
PubChem CID: 11314197
SMILES: C1CCC(CC1)(C2=CC=CC=C2)C(=O)OCCN3CCOCC3.Cl
InChi: InChI=1S/C19H27NO3.ClH/c21-18(23-16-13-20-11-14-22-15-12-20)19(9-5-2-6-10-19)17-7-3-1-4-8-17;/h1,3-4,7-8H,2,5-6,9-16H2;1H
InChi Key: QUJWFJNHTBKCLU-UHFFFAOYSA-N
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |