|1'-(4-(1-(4-氟苯基)-1H-吲哚-3-基)丁基)-3H-螺环[异苯并呋喃-1,4'-哌啶]盐酸盐|CsnPharm

CAS No.: 224177-60-0

Siramesine HCl/西拉美新盐酸盐 Catalog No. CSN16281

Synonyms: Lu 28-179 hydrochloride;Lu 28-179 HCl;Siramesine

Siramesine HCl is an agonist of sigma-2 receptor which can trigger cell death and exhibit anticancer activity.

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生物活性

描述Sigma receptors are ubiquitously expressed in mammals with high levels found in the central nervous system (CNS) and in cancer. There are two subtypes of sigma receptors, sigma-1 and sigma-2. Although sigma-1 receptors promote cell growth and thus inhibit cell death, activation of sigma-2 receptors was reported to trigger cell death^[3]. Siramesine hydrochloride is a selective sigma receptors agonist with IC₅₀s of 17 and 0.12 nM for sigma-1 and sigma-2 receptors, respectively^[4]. In all cell lines tested, the siramesine concentration found to induce significant cell death within 8 h was in the range of 20 -30 μM, whereas 90% of cells were dead after treatment with 40–50 μM siramesine. Six hours post treatment with 25 or 40 μM siramesine, HaCaT cells exhibited characteristic apoptotic morphology with chromatin condensation and apoptotic body formation. In HaCaT cells, significant accumulation of the proforms of cysteine cathepsin L and cathepsins B and C was observed upon treatment with siramesine concentrations ≤15 μM^[3].
参考文献

[1] Cesen MH, Repnik U, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013 Oct 3;4:e818.
[2] Spirkoski J, Melo FR, Grujic M, et al. Mast cell apoptosis induced by siramesine, a sigma-2 receptor agonist. Biochem Pharmacol. 2012 Dec 15;84(12):1671-80.
[3] Česen MH, Repnik U, Turk V, Turk B. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013;4(10):e818
[4] Perregaard J, Moltzen EK, Meier E, Sánchez C. Sigma ligands with subnanomolar affinity and preference for the sigma 2 binding site. 1. 3-(omega-aminoalkyl)-1H-indoles. J Med Chem. 1995;38(11):1998‐2008

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0365 mL
- 10.1825 mL
- 20.3650 mL
- 5 mM
- 0.4073 mL
- 2.0365 mL
- 4.0730 mL
- 10 mM
- 0.2036 mL
- 1.0182 mL
- 2.0365 mL

技术信息

CAS号

224177-60-0

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C30H32ClFN2O

运输

蓝冰

分子量

491.04

别名

Lu 28-179 hydrochloride;Lu 28-179 HCl;Siramesine;Siramesine HCl;Lu-28-179;西拉美新盐酸盐

溶解度

DMSO	98.0 mg/mL (199.6 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (20.4 mM)

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Siramesine HCl/西拉美新盐酸盐 Catalog No. CSN16281

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