| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
PB28 targets the sigma-2 (σ2) receptor as an agonist and the sigma-1 (σ1) receptor as an antagonist. Sigma receptors are involved in various cellular processes, including cell proliferation, apoptosis, and calcium signaling. The σ2 receptor is a potential target for cancer therapy, as it is overexpressed in many tumor cells.
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| 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].
In vitro, PB28 dihydrochloride is a high-affinity σ2 receptor agonist. It displays antiproliferative and cytotoxic effects in SK-N-SH human neuroblastoma and C6 rat glioma cell lines. Its activity is related to its interaction with sigma receptors, leading to cell death in cancer cells. |
| 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].
In vivo, PB28 dihydrochloride shows promise in preclinical models for the treatment of chronic pain and neurodegenerative diseases. As a sigma receptor ligand, it has potential therapeutic applications beyond oncology. However, specific in vivo efficacy data are not detailed in the search results. |
| Enzyme Assay |
The in vitro receptor binding assay for PB28 measures its affinity for σ1 and σ2 receptors. Radioligand binding studies are performed using membrane preparations from tissues or cells expressing these receptors. The compound's ability to compete with a radiolabeled sigma receptor ligand is measured to determine its Ki.
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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. In vitro cellular studies are conducted using cancer cell lines, such as SK-N-SH and C6 cells. Cells are treated with PB28, and cell viability is assessed using MTT or other assays. Apoptosis is measured by detecting caspase activation or using Annexin V staining. The effects on cell cycle progression are also evaluated. |
| 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. In vivo animal experiments for PB28 are performed in models of cancer, pain, or neurodegeneration. Animals are administered PB28, and endpoints such as tumor growth inhibition, pain relief, or neuroprotection are assessed. However, specific protocols are not detailed in the search results. |
| ADME/Pharmacokinetics |
PB28 dihydrochloride has a molecular formula of C24H40Cl2N2O and a molecular weight of 443.49 g/mol. It is soluble in DMSO. For research, it is typically stored at -20°C. Its purity is high (>99%). It is a research-grade compound and is not for human use.
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| Toxicity/Toxicokinetics |
As a potent sigma receptor ligand, PB28 dihydrochloride is not intended for human use as a research chemical. Its toxicological profile is not fully characterized. Standard laboratory safety precautions should be followed. Its effects on cell proliferation and survival are well-documented.
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| References |
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| Additional Infomation |
PB28 dihydrochloride is a high-affinity σ2 receptor agonist and σ1 receptor antagonist. It is a valuable tool for studying the role of sigma receptors in cancer, pain, and neurodegenerative diseases. It is used in research to investigate sigma receptor-mediated signaling and to develop potential therapeutic agents.
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| Molecular Formula |
C24H40CL2N2O
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|---|---|
| Molecular Weight |
443.493205070496
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| Exact Mass |
442.251
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| CAS # |
172907-03-8
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| Related CAS # |
PB28;172906-90-0
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| PubChem CID |
46861545
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
29
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| Complexity |
428
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DSRBJOQIBXACIV-UHFFFAOYSA-N
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| 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
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| Chemical Name |
1-cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine;dihydrochloride
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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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