PB28 (dihydrochloride)

PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity[1][2][3][4][5].

Product Specifications

CAS Number

[172907-03-8]

UNSPSC

12352005

Hazard Statement

H315, H319, H335

Target

Apoptosis; SARS-CoV; Sigma Receptor

Type

Reference compound

Related Pathways

Anti-infection; Apoptosis; Neuronal Signaling

Applications

COVID-19-anti-virus

Field of Research

Cancer; Infection

Assay Protocol

https://www.medchemexpress.com/pb28-dihydrochloride.html

Concentration

10mM

Purity

99.63

Solubility

H2O : 9 mg/mL (ultrasonic; warming) |DMSO : 5 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

[H]Cl.[H]Cl.COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3

Molecular Formula

C24H40Cl2N2O

Molecular Weight

443.49

Precautions

H315, H319, H335

References & Citations

[1]Amalia Azzariti, et al. Cyclohexylpiperazine Derivative PB28, a sigma2 Agonist and sigma1 Antagonist Receptor, Inhibits Cell Growth, Modulates P-glycoprotein, and Synergizes With Anthracyclines in Breast Cancer. Mol Cancer Ther. 2006 Jul;5 (7) :1807-16.|[2]Maria Laura Pati, et al. Sigma-2 Receptor Agonist Derivatives of 1-Cyclohexyl-4-[3- (5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl) propyl]piperazine (PB28) Induce Cell Death via Mitochondrial Superoxide Production and Caspase Activation in Pancreatic Cancer. BMC Cancer. 2017 Jan 13;17 (1) :51.|[3]Nicola A Colabufo, et al. A New Method for Evaluating sigma (2) Ligand Activity in the Isolated Guinea-Pig Bladder. Naunyn Schmiedebergs Arch Pharmacol. 2003 Aug;368 (2) :106-12.|[4]Francesco Berardi, et al. Exploring the Importance of Piperazine N-atoms for sigma (2) Receptor Affinity and Activity in a Series of Analogs of 1-cyclohexyl-4-[3- (5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl) propyl]piperazine (PB28) . J Med Chem. 2009 Dec 10;52 (23) :7817-28.|[5]David E Gordon, et al. A SARS-CoV-2-Human Protein-Protein Interaction Map Reveals Drug Targets and Potential Drug-Repurposing. bioRxiv. 2020 Mar 22;2020.03.22.002386.