[Arg14,Lys15]Nociceptin
[Arg14,Lys15]Nociceptin is a highly potent and selective NOP receptor (ORL1; OP4) agonist, with an EC50 of 1 nM. [Arg14,Lys15]Nociceptin displays high selectivity over opioid receptors, with IC50s of 0.32, 280, >10000 and 1500 nM for NOP, μ, δ and κ receptors, respectively.
For research use only. We do not sell to patients.
- CAS No.: 236098-40-1
- Formula: C82H137N31O22
- Molecular Weight:1909.16
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Opioid Receptor Isoforms
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | EC50 |
1.1 nM
Compound: 1, [RK14-15]Noc
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Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
|
[PMID: 19577933] |
| COS-7 | EC50 |
1.1 nM
Compound: 3, [RK14-15]Noc
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Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
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[PMID: 18818087] |
| COS-7 | IC50 |
0.21 nM
Compound: 1, [RK14-15]Noc
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Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
|
[PMID: 19577933] |
In Vitro
[Arg14,Lys15]Nociceptin is about 30-fold more potent than Nociceptin (NC) and produces longer lasting effects[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 236098-40-1
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Molecular Weight 1909.16
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Formula C82H137N31O22
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Sequence Shortening
FGGFTGARKSARKRKNQ
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Okada K, Sujaku T, Chuman Y, et al. Highly potent nociceptin analog containing the Arg-Lys triple repeat. Biochem Biophys Res Commun. 2000;278(2):493-498. [Content Brief]
[2]. Rizzi D, Rizzi A, Bigoni R, et al. [Arg(14),Lys(15)]nociceptin, a highly potent agonist of the nociceptin/orphanin FQ receptor: in vitro and in vivo studies. J Pharmacol Exp Ther. 2002;300(1):57-63. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)