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R&D Systems™ PIPE 3297 dihydrochloride
SDP

Catalog No. RD10188034 Shop All Novus Products
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RD10188034 5 mg
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Catalog No. RD10188034 Supplier R&D Systems™ Supplier No. 8135/5

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Description

A Tocris product, part of R&D Systems. Potent and selective κ opioid receptor agonist; devoid of β-Arrestin-2 recruitment. Also induces differentiation of OPC.

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% Emax). 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.

Specifications

Chemical Name or Material 3-(2-((1-Benzylazetidin-3-yl)(cyclobutylmethyl)amino)ethyl)phenol dihydrochloride
Quantity 5 mg
Product Line Tocris
Target KOR
Molecular Formula C23H30N2O.2HCl
Purity 98%
Product Title
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