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| 5mg |
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PB28 dihydrochloride, a cyclohexylpiperazine analog, is a novel, high affinity and selective σ2 receptor agonist. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
| ln Vitro |
After 2 days of culture with PB28 dihydrochloride, interfering MCF7 PB28 dihydrochloride induces cell growth through a caspase-independent pathway with IC50s of 25 nM and 15 nM respectively [1]. PB28 dihydrochloride also reduces P-gp expression in a concentration- and time-dependent manner (~60% in MCF7, ~90% in MCF7 ADR) [1]. PB28 dihydrochloride exhibits accumulation in the G0-G1 phase of MCF7 and MCF7 ADR cells, independent of time and concentration [1].
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| ln Vivo |
In Panc02 tumor-burdened mice, treatment with PB28 dihydrochloride (10.7 mg/mL; intraperitoneal injection; daily; weekends; C57BL/6 female mice) suppresses tumor growth. Mice who receive PB28 dihydrochloride also have an advantage in survival [2]. Panc02 cells were implanted into 10 week old female C57BL/6 mice [2].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: MCF7 and MCF7 ADR Cell Tested Concentrations: 25 nM and 15 nM Incubation Duration: 24 hrs (hours), 48 hrs (hours). Experimental Results: Show the cumulative toxicity of MCF7 and MCF7 ADR in the G0-G1 phase [1]. cells independent of time and concentration. |
| Animal Protocol |
Animal/Disease Models: C57BL/6 female mice (10 weeks old) injected with Panc02 cells[2]
Doses: 10.7 mg/mL Route of Administration: intraperitoneal (ip) injection; daily; for two weeks Experimental Results:Inhibited tumor growth in Panc02 tumor burden mice. |
| 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.
[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. |
| Molecular Formula |
C24H40CL2N2O
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|---|---|
| Molecular Weight |
443.493205070496
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| CAS # |
172907-03-8
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| Related CAS # |
PB28;172906-90-0
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
Cl.Cl.COC1=CC=CC2C(CCCC1=2)CCCN1CCN(C2CCCCC2)CC1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~9 mg/mL (~20.29 mM)
DMSO : ~5 mg/mL (~11.27 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2548 mL | 11.2742 mL | 22.5484 mL | |
| 5 mM | 0.4510 mL | 2.2548 mL | 4.5097 mL | |
| 10 mM | 0.2255 mL | 1.1274 mL | 2.2548 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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