1. GPCR/G Protein
    Neuronal Signaling
    Apoptosis
  2. Sigma Receptor
    Ferroptosis
  3. Siramesine hydrochloride

Siramesine hydrochloride (Synonyms: Lu 28-179 hydrochloride)

Cat. No.: HY-14221A Purity: 99.85%
Handling Instructions

Siramesine hydrochloride (Lu 28-179 hydrochloride) 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.

For research use only. We do not sell to patients.

Siramesine hydrochloride Chemical Structure

Siramesine hydrochloride Chemical Structure

CAS No. : 224177-60-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 456 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1080 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

Other Forms of Siramesine hydrochloride:

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Description

Siramesine hydrochloride (Lu 28-179 hydrochloride) 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]

Molecular Weight

491.04

Formula

C₃₀H₃₂ClFN₂O

CAS No.

224177-60-0

SMILES

FC1=CC=C(N2C=C(CCCCN3CCC4(CC3)OCC5=C4C=CC=C5)C6=C2C=CC=C6)C=C1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 42 mg/mL (85.53 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0365 mL 10.1825 mL 20.3649 mL
5 mM 0.4073 mL 2.0365 mL 4.0730 mL
10 mM 0.2036 mL 1.0182 mL 2.0365 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.85%

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

SiramesineLu 28-179Sigma ReceptorFerroptosisInhibitorinhibitorinhibit

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Product Name:
Siramesine hydrochloride
Cat. No.:
HY-14221A
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