PB28 dihydrochloride | Potent sigma2 agonist

CAS:
172907-03-8
Catalog Number:
10-4665
Activity:
High affinity sigma2 ligand
Chemical Names:
1-Cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazine dihydrochloride
Molecular Weight:
443.50
Molecular Formula:
C24H38N2O
Solubility:
Soluble in DMSO (>25 mg/ml) or water (5 mg/ml)
Physical Properties:
White to off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$45.00
25 mg$160.00

PB28 (172907-03-8) is a very potent high affinity (Ki = 5.3 nM1, 0.34 nM2) σ2 agonist.  Selective for σ2 over σ1 (approx 30-40x).1,2 PB28 inhibited cell growth in MCF7 and MCF7 ADR breast cancer cells and displayed strong synergism with doxorubicin.3  PB28 potently inhibited Kv2.1 currents in a σ-independent manner.4 PB28 was recently found to have potent (IC50 = 280 nM) anti-SARS-CoV2 activity.5

References:

  1. Berardi et al. (1996), New s and 5-HT1A Receptor Ligands: w-(Tetralin-1-yl)-n-alkylamine Derivatives; J. Med. Chem. 39 176
  2. Berardi et al. (2004), 4-(Tetralin-1-yl)- and 4-(naphthalen-1-yl)alkyl Derivatives of 1-Cyclohexylpiperazine as s Receptor Ligands with Agonist s2 Activity; J. Med. Chem. 47 2308
  3. Azzariti et al. (2006), Cyclohexylpiperazine derivative PB28, a s2 agonist and s1 antagonist receptor, inhibits cell growth, modulates P-glycoprotein, and synergizes with anthracyclins in breast cancer; Cancer Ther. 5 1807
  4. Liu et al. (2017), Potential independent action of sigma receptor ligands through inhibition of the Kv2.1 channel; Oncotarget 8 59345
  5. Gordon et al. (2020), A SARS-CoV-2 protein interaction map reveals targets for drug repurposing; Nature 583 459
CAS:
172907-03-8
Catalog Number:
10-4665
Activity:
High affinity sigma2 ligand
Chemical Names:
1-Cyclohexyl-4-[3-(1,2,3,4-tetrahydro-5-methoxy-1-naphthalenyl)propyl]piperazine dihydrochloride
Molecular Weight:
443.50
Molecular Formula:
C24H38N2O
Solubility:
Soluble in DMSO (>25 mg/ml) or water (5 mg/ml)
Physical Properties:
White to off-white solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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