NE 100 hydrochloride

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Cat.No. 3133 - NE 100 hydrochloride | C23H33NO2.HCl | CAS No. 149409-57-4
Description: Selective σ1 antagonist
Chemical Name: 4-Methoxy-3-(2-phenylethoxy)-N,N-dipropylbenzeneethanamine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (6)
Reviews
Literature (1)

Biological Activity

Potent and selective σ1 receptor antagonist (Ki = 0.86 nM) that displays > 55-fold selectivity over σ2 receptors and > 6000-fold selectivity over D1, D2, 5-HT1A, 5-HT2 and PCP receptors. Exhibits reversible binding (Kd = 1.2 nM) and displays antipsychotic activity in vivo. Orally active.

Compound Libraries

NE 100 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 391.97
Formula C23H33NO2.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 149409-57-4
PubChem ID 9952420
InChI Key ZHGMDXSHODHWHV-UHFFFAOYSA-N
Smiles CCCN(CCC)CCC1=CC=C(OC)C(OCCC2=CC=CC=C2)=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 9.8 25
DMSO 39.2 100

Preparing Stock Solutions

The following data is based on the product molecular weight 391.97. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.55 mL 12.76 mL 25.51 mL
5 mM 0.51 mL 2.55 mL 5.1 mL
10 mM 0.26 mL 1.28 mL 2.55 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Chaki et al (1994) NE-100, a novel potent σ ligand, preferentially binds to σ1 binding sites in guinea pig brain. Eur.J.Pharmacol. 251 R1 PMID: 8137864

Okuyama et al (1993) NE-100, a novel sigma receptor ligand: in vivo tests. Pharmacol.Letts. 53 PL285

Tanaka et al (1995) Characteristics of binding of [3H]NE-100, a novel sigma-receptor ligand, to guinea-pig brain membranes. Naunyn Schmied.Arch.Pharmacol. 351 244


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Keywords: NE 100 hydrochloride, NE 100 hydrochloride supplier, Selective, σ1, sigma1, antagonists, Receptors, NE100, Sigma1, 3133, Tocris Bioscience

6 Citations for NE 100 hydrochloride

Citations are publications that use Tocris products. Selected citations for NE 100 hydrochloride include:

Fishback et al (2012) A 96-well filtration method for radioligand binding analysis of σ receptor ligands. J Pharm Biomed Anal 71 157 PMID: 22910107

Atzmon et al (2018) Drug Screening Identifies Sigma-1-Receptor as a Target for the Therapy of VWM Leukodystrophy. Front Mol Neurosci 11 336 PMID: 30279648

Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Br J Pharmacol 6 35458 PMID: 26461475

Malik et al (2015) The effects of σ (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice. Int J Neuropsychopharmacol 172 2519 PMID: 25573298


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Literature in this Area

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