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Cat. No.: HY-160761

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K-Opioid receptor agonist-1

K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with K_i of 0.25 nM and EC₅₀ of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone.

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

CAS No.: 1816990-29-0
Formula: C₂₂H₂₉Cl₂N₃O₃
Molecular Weight:454.39

Storage:

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

Data Sheet (269 KB)

K-Opioid receptor agonist-1 Chemical Structure

CAS No.: 1816990-29-0

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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

κ Opioid Receptor/KOR

0.25 nM (Ki)

μ Opioid Receptor/MOR

43 nM (Ki)

δ Opioid Receptor/DOR

58 nM (Ki)

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	2 nM Compound: 5a	Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay Agonist activity at recombinant human kappa-type opioid receptor expressed in HEK293 cells after 30 mins by [35S]GTPgammaS binding assay	[PMID: 28218838]
HEK293	EC₅₀	2 nM Compound: 7b	Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay Agonist activity at kappa opioid receptor in human HEK293 cells after 30 mins by [35S]GTPgammaS binding assay	[PMID: 26411794]

Chemical Information

CAS No. 1816990-29-0
Molecular Weight 454.39
Formula C₂₂H₂₉Cl₂N₃O₃
SMILES

ClC(C=C1CC(N2[C@@]3([H])[C@@](CCC[C@@H]3N4CCCC4)([H])N(CC2)C(OC)=O)=O)=C(C=C1)Cl
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 (269 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]. Soeberdt M, et al., Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. J Med Chem. 2017 Mar 23;60(6):2526-2551. [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.

Bioz

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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K-Opioid receptor agonist-1

All Opioid Receptor Isoforms