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Cat. No.: HY-163277

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PIPE-3297

PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC₅₀ of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity.

For research use only. We do not sell to patients.

Formula: C₂₃H₃₀N₂O
Molecular Weight:350.50

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

PIPE-3297 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

κ Opioid Receptor/KOR

1.1 nM (EC₅₀)

All Opioid Receptor Isoforms :

In Vitro

PIPE-3297 induces myelination and causes oligodendrocyte progenitor cells (OPCs) differentiation into oligodendrocytes (OLs)^[1].
PIPE-3297 exhibits cardiotoxity with 72% hERG inhibition (3 μM) and unstability in liver microsomes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Immunofluorescence^[1]

Cell Line:

OPC
Concentration:

0.5-1 μM
Incubation Time:

72 h
Result:

Increased levels of MBPs

In Vivo

PIPE-3297 (30 mg/kg, s.c., single dosage) leads a KOR occupancy of 90% in CNS and reaches a brain concentration of 12.5 μM. in C57BL/6 mice, reveals no evidence of KOR-mediated hypolocomotion^[1].
PIPE-3297 (30 mg/kg, s.c., single dosage) induces KOR-dependent OPC differentiation into mature OLs in C57BL/6 mice^[1].
PIPE-3297 (3 and 30 mg/kg, s.c., daily for 23 days) ameliorates the autoimmune encephalomyelitis (EAE) induced by myelin oligodendrocyte glycoprotein (MOG) in C57BL/6 mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

MOG induced EAE in C57BL/6 mice^[1]
Dosage:

3 and 30 mg/kg
Administration:

s.c., daily for 23 days
Result:

Ameliorated the EAE.

Animal Model:

C57BL/6 mice^[1]
Dosage:

3 and 30 mg/kg
Administration:

s.c., single dose
Result:

Increased levels of KOR and mature OLs, maintained the locomotion ability.

Chemical Information

Molecular Weight 350.50
Formula C₂₃H₃₀N₂O
SMILES

OC1=CC=CC(CCN(C2CN(C2)CC3=CC=CC=C3)CC4CCC4)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Schrader TO,et al., 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 Feb 7;15(3):685-698. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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