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Key Documents

P9246

Sigma-Aldrich

PB28 dihydrochloride

≥98% (HPLC), solid

Synonym(s):

1-Cyclohexyl-4-(3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)-n-propyl)piperazine dihydrochloride

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About This Item

Linear Formula:
C24H40Cl2N2O
CAS Number:
Molecular Weight:
443.49
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

solid

storage condition

desiccated

color

white

solubility

H2O: ~10 mg/mL at 60 °C

SMILES string

Cl[H].Cl[H].COc1cccc2C(CCCN3CCN(CC3)C4CCCCC4)CCCc12

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

InChI key

DSRBJOQIBXACIV-UHFFFAOYSA-N

Application

PB28 dihydrochloride has been used to test its inhibitory effect on potassium voltage-gated channel, shab-related subfamily, member 1, Kv2.1.

Biochem/physiol Actions

PB28, a cyclohexylpiperazine derivative, is a sigma 1 (σ1)-R antagonist. It elicits anti-tumor activity in breast, ovarian and colorectal cancer cell lines.
Selective σ2 opioid receptor ligand; putative σ2 agonist

Pictograms

Exclamation mark

Signal Word

Warning

Hazard Statements

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

Target Organs

Respiratory system

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US), Eyeshields, Gloves

Certificates of Analysis (COA)

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Xinying Liu et al.
Oncotarget, 8(35), 59345-59358 (2017-09-25)
The sigma-1 receptor (σ1-R) and sigma-2 receptor (σ2-R) are potential drug targets for treatment of cancer, pain, depression, retinal degeneration and other neuronal diseases. Previous reports show that sigma-1 receptor modulates the activities of multiple channels. We are interested in
Nicola A Colabufo et al.
Naunyn-Schmiedeberg's archives of pharmacology, 368(2), 106-112 (2003-07-25)
We demonstrated the presence of sigma(2) receptors in the guinea-pig ileum by saturation analysis and extended our investigation to guinea-pig bladder and rat bladder. In functional assays of the isolated tissues in organ baths, sigma(2) receptor ligands inhibited electrically evoked
Nicola Antonio Colabufo et al.
Cancer letters, 237(1), 83-88 (2005-07-12)
Sigma2 (sigma2) receptor proteins are overexpressed in several tissues and tumour cell lines. Although the biomolecular mechanism of this overexpression must be elucidated, sigma2 receptor was considered a potential biomarker for monitoring solid tumour proliferation. In this study, we verified
Evangelia Sereti et al.
Biomedicines, 9(1) (2021-01-21)
Sigma (σ) receptors have attracted great interest since they are implicated in various cellular functions and biological processes and diseases, including various types of cancer. The receptor family consists of two subtypes: sigma-1 (σ1) and sigma-2 (σ2). Both σ receptor

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