PB 28 dihydrochloride

Category	SARS-CoV
CAS	172907-03-8
Description	PB 28 dihydrochloride is a high affinity σ2 receptor agonist. It displays antiproliferative and cytotoxic effects in SK-N-SH neuroblastoma and C6 glioma cells.

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Product Information

Synonyms	PB 28 dihydrochloride; PB28 dihydrochloride; PB-28 dihydrochloride; 1-Cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazine dihydrochloride
Molecular Weight	443.5
Molecular Formula	C24H38N2O.2HCl
Canonical SMILES	CC1=CC(=O)N(C(=O)C1=C(C)NC2=CC=CC=C2N)O.Cl.Cl
InChI	InChI=1S/C14H15N3O3.2ClH/c1-8-7-12(18)17(20)14(19)13(8)9(2)16-11-6-4-3-5-10(11)15;;/h3-7,16,20H,15H2,1-2H3;2*1H/b13-9+;;
InChIKey	FKMUQHJGHGZYLC-IGUOPLJTSA-N
Purity	≥99% by HPLC
Solubility	In vitro: 10 mM in DMSO
Appearance	White to off-white (Solid)
Storage	4°C, sealed storage, away from moisture * In solvent : -80°C, 6 months -20°C, 1 month (sealed storage, away from moisture)
Complexity	428
Exact Mass	442.2517693
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 Ki (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.
In Vivo	PB28 (10.7 mg/mL; intraperitoneal injection; daily; for two weeks; C57BL/6 female mice) treatment inhibits tumor growth in Panc02 tumor burden mice. PB28 also conferres a survival advantage for mice. 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.
PSA	15.71000
Target	Ki: 0.68 nM (σ2 receptor); 0.38 nM (σ1 receptor)