2. Neuronal Signaling Apoptosis
  3. Sigma Receptor Ferroptosis
  4. Siramesine hydrochloride

Siramesine hydrochloride  (Synonyms: Lu 28-179 hydrochloride)

Cat. No.: HY-14221A Purity: 99.74%
COA Handling Instructions

Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity.

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Siramesine hydrochloride Chemical Structure

Siramesine hydrochloride Chemical Structure

CAS No. : 224177-60-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 151 In-stock
Solution
10 mM * 1 mL in DMSO USD 151 In-stock
Solid
1 mg USD 70 In-stock
2 mg USD 100 In-stock
5 mg USD 140 In-stock
10 mg USD 225 In-stock
25 mg USD 450 In-stock
50 mg USD 740 In-stock
100 mg USD 1180 In-stock
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Based on 4 publication(s) in Google Scholar

Other Forms of Siramesine hydrochloride:

Siramesine hydrochloride Related Antibodies

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Description

Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity[1][2][3].

In Vitro

Siramesine hydrochloride displays the binding affinities: 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, IC50 (alpha 1)=330 nM[1].
Siramesine (0-50μM; 8 hours) hydrochloride induces cell death in various cell lines (HaCaT, Hsc-4, HeLa and MCF-7, neuroblastoma cell line SH-SY5Y and glioblastoma cell line U-87MG)[2].
Siramesine (0-40 μM; 2-48 hours) hydrochloride activates caspases in HaCaT and in U-87MG cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Siramesine hydrochloride Related Antibodies
Molecular Weight

491.04

Appearance

Solid

Formula

C30H32ClFN2O
CAS No.
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.74%

COA (251 KB) LCMS (269 KB)

Handling Instructions (2659 KB)
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Siramesine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Siramesine224177-60-0Lu 28-179Sigma ReceptorFerroptosiscancerselectivitydeathcathepsinmitochondrialysosomesInhibitorinhibitorinhibit

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