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PB28

CAT: 0804-HY-108511ASize: 1 EachDry Ice: NoHazardous: No
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Description
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity[1][2][3][4][5].
CAS Number
172906-90-0
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.html
Solubility
10 mM in DMSO
Smiles
COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3
Molecular Formula
C24H38N2O
Molecular Weight
370.57
Precautions
P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P362+P364-P403+P233-P405-P501
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Sigma 1 Receptor; Sigma 2 Receptor

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