PIPE 3297 dihydrochloride

Key Product Details

Product Description

PIPE 3297 dihydrochloride is a potent and selective agonist of κ opioid receptor (KOR). It potently activates G-protein signaling (GTPγS EC₅₀ = 1.1 nM, 91% E_max). It displays 40- and 600- fold selectivity over MOR and DOR respectively.

PIPE 3297 dihydrochloride induces differentiation of oligodendrocyte progenitor cells (OPC) in vitro and in vivo, leading to significant increase of mature oligodendrocytes (OL) in healthy mice and inducing myelination. It also reduces disease score in mouse experimental autoimmune encephalomyelitis (EAE) model. Exhibits low β-arrestin2 recruitment activity, avoding the sedating effects typically associated to other KOR agonists employed in demyelinating diseases.

PIPE 3297 dihydrochloride is brain penetrant and leads to 90% occupancy in CNS in vivo (mouse).

PIPE 3297 exhibits cardiotoxity with 72% hERG inhibition (3 μM) and unstability in liver microsomes.

Product Specifications for PIPE 3297 dihydrochloride

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for PIPE 3297 dihydrochloride

The following data is based on the product molecular weight 423.42.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.36 mL	11.81 mL	23.62 mL
5 mM	0.47 mL	2.36 mL	4.72 mL
10 mM	0.24 mL	1.18 mL	2.36 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Schrader Identification and in vivo evaluation of myelination agent PIPE-3297, a selective kappa opioid receptor agonist devoid of β-Arrestin-2 recruitment efficacy. ACS Chem.Neurosci. 2024 PMID: 38265210

Product Documents for PIPE 3297 dihydrochloride