| Identification | Back Directory | [Name]
AC-ARG-TYR-TYR-ARG-ILE-LYS-NH2 | [CAS]
200959-48-4 | [Synonyms]
Ac-RYYRIK-NH
AC-RYYRIK-NH2
Ac-RYYRIK amide
ACETYL-RYYRIK, AMIDE
AC-ARG-TYR-TYR-ARG-ILE-LYS-NH2
N2-Acetyl-L-arginyl-L-tyrosyl-L-tyrosyl-L-arginyl-L-isoleucyl-L-lysinamide
L-Lysinamide, N2-acetyl-L-arginyl-L-tyrosyl-L-tyrosyl-L-arginyl-L-isoleucyl- | [Molecular Formula]
C44H70N14O9 | [MDL Number]
MFCD02262126 | [MOL File]
200959-48-4.mol | [Molecular Weight]
939.11 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
-15°C
| [solubility ]
Soluble in Chloroform,Dichloromethane,Ethyl Acetate,DMSO,Acetone,etc. | [form ]
Powder | [pka]
9.82±0.15(Predicted) |
| Hazard Information | Back Directory | [Uses]
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[1]. | [Biological Activity]
Ac-RYYRIK-NH2 is a potent ORL1 partial agonist as an endogenous ligand of ORL1 in CHO cells (Kd=1.5 nM). Ac-RYYRIK-NH2 is a specific antagonist of G protein activation and competitively antagonizes noc/OFQ-stimulated [35S]-GTPgS-binding G protein in rat meninges and brain sections. | [in vivo]
Ac-RYYRIK-NH2 (intracerebroventricularly (icv) inhibits spontaneous locomotor activity in mice with an ID 50 of 0.07 nmol. Co-administration of noc/OFQ and Ac-RYYRIK-NH2 | [target]
Kd: 1.5 nM (ORL1 transfected in CHO cells) | [storage]
Desiccate at -20°C | [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. DOI:10.1038/sj.bjp.0702353
[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. DOI:10.1016/s0196-9781(00)00251-5
[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. PMID:9353393 |
|
|