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Siramesine hydrochloride, Lu-28-179 CAS NO.224177-60-0
- FOB Price: USD: 1.00-1.00 /Gram Get Latest Price
- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- Siramesine hydrochloride, Lu-28-179
- SiraMesine, Lu-28-179;SiraMesine (hydrochloride);1'-[4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl]spiro[isobenzofuran-1(3H),4'-piperidine] monohydrochloride;Siramesine (HCl salt), Lu-28-179;Siramesine hy
- 224177-60-0
Quick Details
- ProName: Siramesine hydrochloride, Lu-28-179
- CasNo: 224177-60-0
- Molecular Formula: C30H32ClFN2O
- Appearance: white solid
- Application: CAS：224177-60-0； Small molecule inhib...
- DeliveryTime: 2 months
- PackAge: 100g,500g,1kg,25kg/drum
- Port: shang hai
- ProductionCapacity: 1000 Gram/Week
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
We are committed to provide excellence in researching, manufacturing and drug discovery process.
Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
Siramesine(Lu 28-179) Hcl is a selective sigma-2 receptor agonist, which has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo.
IC50 value:
Target: sigma-2 receptor; lysosome-destabilizing agent
siramesine can induce rapid cell death in a number of cell lines at concentrations above 20 μM. In HaCaT cells, cell death was accompanied by caspase activation, rapid loss of mitochondrial membrane potential (MMP), cytochrome c release, cardiolipin peroxidation and typical apoptotic morphology, whereas in U-87MG cells most apoptotic hallmarks were not notable, although MMP was rapidly lost [1]. Siramesine, a sigma-2 receptor agonist originally developed as an anti-depressant, can induce cell death in transformed cells through a mechanism involving lysosomal destabilization [2].
in vivo: SA4503 or siramesine given jointly with MEM (as well as with AMA) decreased the immobility time in rats. The effect of SA4503 and AMA co-administration was antagonized by progesterone, a sigma1 receptor antagonistic neurosteroid. Combined treatment with siramesine and AMA was modified by neither progesterone nor BD1047 (a novel sigma antagonist with preferential affinity for sigma1 sites) [3]