PB28 dihydrochloride (Standard)
PB28 dihydrochloride (Standard) is the analytical standard of PB28 (dihydrochloride) (HY-108511). This product is intended for research and analytical applications. 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.
For research use only. We do not sell to patients.
- CAS No.: 172907-03-8
- Formula: C24H40Cl2N2O
- Molecular Weight:443.49
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Product Information
The compound is the grade of analytical standard, which is the reference standard supplied assay. It is commonly used in qualitative, quantitative and methodological research experiments in HPLC, GC and MS.
Chemical Information
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CAS No. 172907-03-8
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Molecular Weight 443.49
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Formula C24H40Cl2N2O
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SMILES
[H]Cl.[H]Cl.COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)