S1RA (E-52862) | B3048

S1RA is a highly selective sigma-1 (σ1) receptor antagonist. It shows high affinity for σ1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig σ1 receptors respectively but no significant affinity for the σ2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat σ2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.

S1RA is a highly selective sigma-1 (σ1) receptor antagonist. It shows high affinity for σ1 receptors with Ki values of 17 nM and 23.5 nM for human and guinea pig σ1 receptors respectively but no significant affinity for the σ2 receptors with Ki values of 1000 nM and 9300 nM for guinea pig and rat σ2 receptors respectively. It shows moderate affinity (Ki = 328 nM) and antagonistic activity with low potency at the human 5-HT2B receptor. S1RA inhibits neuropathic pain in formalin-induced nociception and capsaicin-induced mechanical hypersensitivity in mice. Sigma receptor modulators may show activity against SARS-CoV-2 as sigma receptors interact with SARS-CoV-2 proteins Nsp6 and Orf9c.

B3048 | S1RA (E-52862) DataSheet

Alternate Name/Synonyms: 4-[2-(5-methyl-1-naphthalen-2-ylpyrazol-3-yl)oxyethyl]morpholine; sigma 1 receptor antagonist

Appearance: A crystalline solid

Formulation:

CAS Number: 878141-96-9

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₂₀H₂₃N₃O₂

Molecular Weight: 337.42

Cell-Permeable?: FALSE

Purity: ≥98%

Solubilities: ~10 mg/ml in DMF, ~1 mg/ml in ethanol, ~15 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: A highly selective sigma-1 (σ1) receptor antagonist

MDL Number: MFCD25976945

PubChem CID: 44247568

SMILES: CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4

InChi: InChI=1S/C20H23N3O2/c1-16-14-20(25-13-10-22-8-11-24-12-9-22)21-23(16)19-7-6-17-4-2-3-5-18(17)15-19/h2-7,14-15H,8-13H2,1H3

InChi Key: DGPGXHRHNRYVDH-UHFFFAOYSA-N