Siramesine (hydrochloride)
CAS No. : 224177-60-0
(Synonyms: Lu 28-179 (hydrochloride))
| Size | Price | Stock |
|---|---|---|
| 2mg | $100 | In-stock |
| 5mg | $140 | In-stock |
| 10mg | $225 | In-stock |
| 25mg | $450 | In-stock |
| 50mg | $740 | In-stock |
| 100mg | $1180 | In-stock |
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| Cat. No. : | HY-14221A |
| M.Wt: | 491.04 |
| Formula: | C30H32ClFN2O |
| Purity: | >98 % |
| Solubility: | DMSO : ≥ 42 mg/mL |
Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3].
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[1].
Siramesine (0-50μM; 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)[2].
Siramesine (0-40 μM; 2-48 hours) hydrochloride activates caspases in HaCaT and in U-87MG cells[2].
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