PB 28 dihydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	172907-03-8
包装:	10mg
市场价:	3120元

产品介绍

化学性质

Physical Appearance	White solid
Storage	Store at 4°C
M.Wt	443.5
Cas No.	172907-03-8
Formula	C₂₄H₃₈N₂O·2HCl
Solubility	<8.87mg/ml in H2O
Chemical Name	1-cyclohexyl-4-(3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl)piperazine dihydrochloride
Canonical SMILES	COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3.Cl.Cl
运输条件	蓝冰运输或根据您的需求运输。
一般建议	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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

PB 28 dihydrochloride, a cyclohexylpiperazine derivative, is sigma (σ) receptor ligand, acting as a σ₂receptor agonist with a Ki value of 0.68 nM, as well as a σ₁receptor antagonist with a Ki of 0.38 nM. The σ receptor, composed of σ₁and σ₂subtypes, is present with high density in central nervous system and peripheral organs, and overexpressed in many tumor cell lines. Selective σ₂receptor agonists have been proposed as anticancer drugs, while selective σ₁receptor ligands have been proposed to develop new classes of central nervous system agents for neuroprotection, anxiety, depression, psychosis, as well as learning and memory improvement.

References:

1. Berardi F, Abate C, Ferorelli S, 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). Journal of Medicinal Chemistry, 2009, 52(23): 7817-7828.

2. Azzariti A, Colabufo NA, Berardi F, 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. Molecular Cancer Therapeutics, 2006, 5(7): 1807-1816.

3. Pati ML, Hornick JR, Niso M, 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, 17(1): 51.

试验操作

Cell experiment:[2]
Cell lines	Human breast cancer cell lines, MCF7 and MCF7 ADR (resistant to Adriamycin or doxorubicin)
Reaction Conditions	25 and 15 nM PB 28 dihydrochloride for 2 d incubation
Applications	PB 28 dihydrochloride inhibited growth of MCF-7 and multidrug-resistant MCF7 ADR cells, with IC50 values being 25 and 15 nM, respectively. PB 28 dihydrochloride also decreased basal P-glycoprotein levels in the same cells.
Animal experiment:[2]
Animal models	C57BL/6 mice bearing Panc02 tumors
Dosage form	10.7 mg/mL Once daily by intraperitoneal injection for 2 weeks
Applications	PB 28 dihydrochloride treatment inhibited tumor growth in Panc02 tumor burden mice. Even though treatment was discontinued (on day 15), PB 28 dihydrochloride also conferred a survival advantage for mice in this experiment.
Note	The technical data provided above is for reference only.
	References: 1. Berardi F, Abate C, Ferorelli S, 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). Journal of Medicinal Chemistry, 2009, 52(23): 7817-7828. 2. Azzariti A, Colabufo NA, Berardi F, 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. Molecular Cancer Therapeutics, 2006, 5(7): 1807-1816. 3. Pati ML, Hornick JR, Niso M, 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, 17(1): 51.