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PB28 (dihydrochloride)

PB28 (dihydrochloride)

Item no.	HY-108511-50mg
Manufacturer	MedChem Express
CASRN	172907-03-8
Amount	50 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 1 mg 25 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitor
Specific against	other
Purity	99.63
Citations	[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.
Smiles	[H]Cl.[H]Cl.COC1=CC=CC2=C1CCCC2CCCN3CCN(C4CCCCC4)CC3
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	COVID-19-anti-virus
Manufacturer - Targets	Apoptosis; SARS-CoV; Sigma Receptor
Shipping Temperature	Room Temperature
Storage Conditions	4°C (Powder, sealed storage, away from moisture)
Molecular Weight	443.49
Product Description	PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki 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[1][2][3][4][5].
Manufacturer - Research Area	Cancer; Infection
Solubility	H2O: 9 mg/mL (ultrasonic; warming)\|DMSO: 5 mg/mL (ultrasonic; warming; heat to 60°C)
Manufacturer - Pathway	Anti-infection; Apoptosis; Neuronal Signaling
Isoform	Sigma 1 Receptor; Sigma 2 Receptor
Clinical information	No Development Reported

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HY-108511-50mg-safety-datasheet.pdf