S1RA
CAS No. : 878141-96-9
(Synonyms: E-52862)
| Size | Price | Stock |
|---|---|---|
| 5mg | $90 | In-stock |
| 10mg | $165 | In-stock |
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| Cat. No. : | HY-18099 |
| M.Wt: | 337.42 |
| Formula: | C20H23N3O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 33.33 mg/mL (ultrasonic;warming;heat to 60°C);1M HCl : 50 mg/mL (ultrasonic;adjust pH to 1 with HCl) |
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice[1][2].
In Vitro:S1RA (E-52862; 100 µM; 4 h) inhibit intracellular calcium responses in TRPA1 expressing HEK293 cells[2].
S1RA (100 µM; 4 h) impairs the formation of TRPA1–Sigma-1R complexes and reduces TRPA1 expression at the plasma membrane[2].
In Vivo:S1RA (E-52862; 40 mg/kg; IP; single dose) produces a substantial reduction in pain-related responses to intradermal Allylisothiocyanate (AITC) in WT mice[2].
S1RA (40 mg/kg; IP; once a day for 11 consecutive days; starting 3 days before Oxaliplatin injection) prevents mechanical and cold hypersensitivity in Oxaliplatin (6 mg/kg; i.p.; Day 0, Day 2, Day 4)-treated mice[2].
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