Ac-RYYRIK-NH2
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain.
For research use only. We do not sell to patients.
- CAS No.: 200959-48-4
- Formula: C44H70N14O9
- Molecular Weight:939.11
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Kd: 1.5 nM (ORL1 transfected in CHO cells)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
1.04 nM
Compound: Ac-RYYRIK-NH2
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Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
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[PMID: 25284251] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 200959-48-4
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Molecular Weight 939.11
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Formula C44H70N14O9
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Sequence Shortening
Ac-RYYRIK-NH2
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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]. H Berger, et al. Antagonism by acetyl-RYYRIK-NH2 of G protein activation in rat brain preparations and of chronotropic effect on rat cardiomyocytes evoked by nociceptin/orphanin FQ. Br J Pharmacol. 1999 Feb;126(3):555-8. [Content Brief]
[2]. H Berger, et al. The nociceptin/orphanin FQ receptor ligand acetyl-RYYRIK-amide exhibits antagonistic and agonistic properties.Peptides. 2000 Jul;21(7):1131-9. [Content Brief]
[3]. C T Dooley, et al. Binding and in vitro activities of peptides with high affinity for the nociceptin/orphanin FQ receptor, ORL1. J Pharmacol Exp Ther. 1997 Nov;283(2):735-41. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ac-RYYRIK-NH2 Related Classifications
HY-P1318 Related Classifications
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