Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Formerly known as Lu-28-179, siramesine HCl is a potent and selective sigma-2 receptor agonist with anticancer effects. Siramesine is able to trigger cancer cell death through destabilisation of mitochondria and exhibit promising anticancer activity in vivo. 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.
ln Vitro |
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, and IC50 (alpha 1) = 330 nM are the binding affinities displayed by simeimesine hydrochloride[1]. In different cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y, and glioblastoma cell line U-87MG), siramesine hydrochloride (0-50μM; 8 hours) induces cell death[2]. In HaCaT and U-87MG cells, siramesine hydrochloride (0–40 μM; 2-48 hours) activates caspases[2].
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ln Vivo |
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Animal Protocol |
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References |
Cell Death Dis.2013 Oct 3;4:e818.
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Molecular Formula |
C30H32CLFN2O
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Molecular Weight |
491.05
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CAS # |
224177-60-0
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Related CAS # |
Siramesine;147817-50-3;Siramesine fumarate;163630-79-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=CC=CC=C45)C6=C2C=CC=C6)C=C1.[H]Cl
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0365 mL | 10.1823 mL | 20.3645 mL | |
5 mM | 0.4073 mL | 2.0365 mL | 4.0729 mL | |
10 mM | 0.2036 mL | 1.0182 mL | 2.0365 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Effect of siramesine on viability of various cell lines.Cell Death Dis.2013 Oct 3;4:e818. th> |
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Effect of siramesine on mitochondria.Cell Death Dis.2013 Oct 3;4:e818. td> |
ROS generation in siramesine-induced cell death.Cell Death Dis.2013 Oct 3;4:e818. td> |