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Cat. No.: HY-144610

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Mu opioid receptor antagonist 5

Mu opioid receptor antagonist 5 (compound NAP) is a selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with an EC₅₀ value of 1.14 nM and a K_i value of 0.37 nM. Mu opioid receptor antagonist 5 can be used for researching opioid use disorders (OUD).

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

CAS No.: 1124167-61-8
Formula: C₂₆H₂₉N₃O₄
Molecular Weight:447.53

Storage:

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

Data Sheet (273 KB)

Mu opioid receptor antagonist 5 Chemical Structure

CAS No.: 1124167-61-8

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

μ Opioid Receptor/MOR

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1.14 nM Compound: 6, NAP	Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Activity at monocloned mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 19199782]
CHO	IC₅₀	1.61 nM Compound: 6, NAP	Binding affinity to mu opioid Y210A mutant receptor expressed in CHO cells Binding affinity to mu opioid Y210A mutant receptor expressed in CHO cells	[PMID: 19199782]
CHO	IC₅₀	2.29 nM Compound: 6, NAP	Binding affinity to wild type mu opioid receptor expressed in CHO cells Binding affinity to wild type mu opioid receptor expressed in CHO cells	[PMID: 19199782]
CHO	IC₅₀	>1000 nM Compound: 6, NAP	Binding affinity to mu opioid W318A mutant receptor expressed in CHO cells Binding affinity to mu opioid W318A mutant receptor expressed in CHO cells	[PMID: 19199782]
CHO	EC₅₀	15.2 nM Compound: NAP	Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding Agonist activity at delta opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding	[PMID: 23116124]
CHO	EC₅₀	28.8 nM Compound: NAP	Agonist activity at kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding Agonist activity at kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]-GTP-gammaS binding	[PMID: 23116124]
CHO	IC₅₀	1.61 nM Compound: NAP	Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay Binding affinity to MOR Y210A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	[PMID: 24055076]
CHO	IC₅₀	2.29 nM Compound: NAP	Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay Binding affinity to wild type MOR (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	[PMID: 24055076]
CHO	IC₅₀	>1000 nM Compound: NAP	Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay Binding affinity to MOR W318A mutant (unknown origin) expressed in CHO cells after 15 mins by Ca2+ mobilization assay	[PMID: 24055076]

Chemical Information

CAS No. 1124167-61-8
Molecular Weight 447.53
Formula C₂₆H₂₉N₃O₄
SMILES

O[C@]12[C@H]3CC4=C5[C@@]1(CCN3CC6CC6)[C@H]([C@@H](CC2)NC(C7=CC=NC=C7)=O)OC5=C(O)C=C4
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]. Pagare PP, et al. Design, Synthesis, and Biological Evaluation of NAP Isosteres: A Switch from Peripheral to Central Nervous System Acting Mu-Opioid Receptor Antagonists. J Med Chem. 2022;65(6):5095-5112. [Content Brief]

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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.

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100 mg

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