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Product Details

PB28 dihydrochloride | High Affinity sigma 2 ligand / Anti-SARS-CoV2

PB28 (172907-03-8) is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist. Selective for σ2 over σ1 (approx 30-40x).1,2 PB28 inhibited cell growth in MCF7 and MCF7 ADR breast cancer cells and displayed strong synergism with doxorubicin.3 PB28 potently inhibited Kv2.1 currents in a σ-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5

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References/Citations

1) Berardi et al. (1996), New σ and 5-HT1A Receptor Ligands: ω-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176
2) Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as σ Receptor Ligands with Agonist σ2 Activity; J. Med. Chem. 47 2308
3) Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a σ2 agonist and σ1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclins in breast cancer; Mol. Cancer Ther. 5 1807
4) Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345
5) Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459

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Focus Biomolecules cell signaling reagent supplier, chemical structure of PB28 | Sigma 2 lignad/Anti SARS-CoV2 | CAS

Catalog#  10-4665-0005

$45.00
Quantity
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CAS:
172907-03-8
Catalog Number:
10-4665
Activity:
High affitity σ2 ligand / anti-SARS-CoV2
Chemical Name:
1-Cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazine dihydrochloride
Molecular Weight:
443.50
Molecular Formula:
C24H38N2O • 2HCl
Solubility:
Soluble in DMSO (up to at least 25 mg/ml) or in Water (up to 5 mg/ml).
Physical Properties:
White or off-white solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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