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首页-小分子抑制剂&激动剂-GPCR-Sigma Receptor-Siramesine
Siramesine

Chemical Structure : Siramesine

CAS No.: 147817-50-3

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Siramesine (Lu 28-179, Lu28-179)

货号: PC-28288Not For Human Use, Lab Use Only.

Siramesine (Lu 28-179) is a lysosomotropic agent and potent, selective sigma-2 receptor ligand and agonist with binding IC50 of 0.12 nM, exhibits 140-fold selectivity over Sigma-1 receptor.

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5 mg ￥980 In stock
10 mg ￥1480 In stock
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Siramesine (Lu 28-179) is a lysosomotropic agent and potent, selective sigma-2 receptor ligand and agonist with binding IC50 of 0.12 nM, exhibits 140-fold selectivity over Sigma-1 receptor.
Siramesine inhibits acid sphingomyelinase (ASM) by interfering with the binding of ASM to its essential lysosomal cofactor, bis(monoacylglycero)phosphate.
Siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation.
Siramesine induces lysosomal leakage and cathepsin-dependent death of cancer cells in vitro and displays potent anti-cancer activity in vivo.
Siramesine effectively induces caspase-independent programmed cell death in immortalized and transformed cells of various origins.

物理化学性质&存储条件

分子量 454.59
分子式 C30H31FN2O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1'-(4-(1-(4-Fluorophenyl)-1H-indol-3-yl)butyl)-3H-spiro[isobenzofuran-1,4'-piperidine]

参考文献

1. Česen MH, et al. Cell Death Dis. 2013 Oct 3;4(10):e818.

2. Petersen NH, et al. Cancer Cell. 2013 Sep 9;24(3):379-93.

3. Zeng C, et al. Br J Cancer. 2012 Feb 14;106(4):693-701.

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