PB 28 dihydrochloride|172907-03-8|-陌孚医药/Medlife

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PB 28 dihydrochloride

目录号: PC11252 纯度: ≥98%

CAS No. :172907-03-8

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中文名称	PB 28 dihydrochloride
中文别名	1-环己基-4-[3-(1,2,3,4-四氢-5-甲氧基-1-萘基)丙基]哌嗪二盐酸盐
英文名称	PB 28 dihydrochloride
英文别名	PB 28 dihydrochloride
Cas No.	172907-03-8
分子式	C₂₄H₄₀Cl₂N₂O
分子量	443.49
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a K_i 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.

性状

Solid

体外研究(In Vitro)

PB28 (15-25 nM; 24-48 hours; MCF7 and MCF7 ADR cells) dihydrochloride treatment shows an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that are time and concentration independent.
PB28 dihydrochloride has a higher σ2 receptor affinity expressed as K_i (0.28 nM and 0.17 nM in MCF7 and MCF7 ADR cells, respectively) than σ1 receptor affinity (13.0 nMand 10.0 nM, respectively).
PB28 dihydrochloride inhibits cell growth of MCF7 and MCF7 ADR cells with IC₅₀s of 25 nM and 15 nM, respectively after 2-day treatment.
PB28 dihydrochloride induces apoptosis through a caspase-independent pathway.
PB28 dihydrochloride also reduces P-gp expression in a concentration- and time-dependent manner (approximately 60% in MCF7 and 90% in MCF7 ADR).
PB28 dihydrochloride displays antiproliferative and cytotoxic effects in both C6 rat glioma and SK-N-SH human neuroblastoma cell lines.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	MCF7 and MCF7 ADR cells
Concentration:	25 nM and 15 nM
Incubation Time:	24 hours, 48 hours
Result:	Showed an accumulation in the G0-G1 phase for MCF7 and MCF7 ADR cells that were time and concentration independent.

体内研究(In Vivo)

PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) dihydrochloride treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 female mice (10 weeks old) injected with Panc02 cells
Dosage:	10.7 mg/mL
Administration:	Intraperitoneal injection; daily; for two weeks
Result:	Inhibited tumor growth in Panc02 tumor burden mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

[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. [Information]

[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. [Information]

[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. [Information]

[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 [Information]

[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. [Information]

溶解度数据

体外研究:

H₂O : 9 mg/mL (20.29 mM; Need ultrasonic and warming)

DMSO : 5 mg/mL (11.27 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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