A σ receptor ligand with anticancer and antiviral activities
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PB 28 (hydrochloride)

Item No. 31742

Technical Information
Formal Name
1-cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]-piperazine, dihydrochloride
CAS Number
172907-03-8
Molecular Formula
C24H38N2O • 2HCl
Formula Weight
Purity
≥98%
A crystalline solid
Methanol: solubleWater: soluble
SMILES
COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3.Cl.Cl
InChi Code
InChI=1S/C24H38N2O.2ClH/c1-27-24-14-6-12-22-20(8-5-13-23(22)24)9-7-15-25-16-18-26(19-17-25)21-10-3-2-4-11-21;;/h6,12,14,20-21H,2-5,7-11,13,15-19H2,1H3;2*1H
InChi Key
DSRBJOQIBXACIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    PB 28 is a sigma (σ) receptor ligand that binds to σ1 and σ2 receptors (Kis = 13 and 0.28 nM, respectively, in MCF-7 cell membranes) with anticancer and antiviral activities.1,2 It is selective for σ1 and σ2 receptors over human ether-a-go-go (hERG) channels (Ki = 1,000 nM).2 PB 28 inhibits growth of MCF-7 and multidrug-resistant MCF-7/adr cells (IC50s = 25 and 15 nM, respectively).1 It also decreases basal P-glycoprotein (P-gp) levels in the same cells. PB 28 reduces severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infectivity in Vero E6 cells (IC90 = 278 nM), which is 20 times more potent than hydroxychloroquine (Item No. 17911).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Azzariti, A., Colabufo, N.A., Beradi, F., et alCyclohexylpiperazine derivative PB28, a σ2 agonist and σ1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclines in breast cancer. Mol. Cancer Ther. 5(7), 1807-1816 (2006).

    2. Gordon, D.E., Jang, G.M., Bouhaddou, M., et alA SARS-CoV-2 protein interaction map reveals targets for drug repurposing. Nature 583(7816), 459-468 (2020).