CAS 200959-48-4|Ac-RYYRIK-NH2 TFA

Introduction:Basic information about CAS 200959-48-4|Ac-RYYRIK-NH2 TFA, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameAc-RYYRIK-NH2 TFA
CAS Number200959-48-4Molecular Weight939.115
Density1.4±0.1 g/cm3Boiling Point/
Molecular FormulaC44H70N14O9Melting Point/
MSDSUSAFlash Point/

Names

NameAc-RYYRIK-NH2
SynonymMore Synonyms

Ac-RYYRIK-NH2 TFA BiologicalActivity

DescriptionAc-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].
Related CatalogSignaling Pathways >>GPCR/G Protein >>Opioid ReceptorSignaling Pathways >>Neuronal Signaling >>Opioid ReceptorResearch Areas >>Neurological Disease
Target

Kd: 1.5 nM (ORL1 transfected in CHO cells)[1]

In VivoAc-RYYRIK-NH2 (intracerebroventricularly (i.c.v.) inhibits spontaneous locomotor activity in mice with an ID50 of 0.07 nmol. Co-administration of noc/OFQ and Ac-RYYRIK-NH2 lead to additive effects in Male Swiss mice[1].
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.

[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.

[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.

Chemical & Physical Properties

Density1.4±0.1 g/cm3
Molecular FormulaC44H70N14O9
Molecular Weight939.115
Exact Mass938.545044
PSA407.97000
LogP-1.04
Index of Refraction1.644
InChIKeyWBBBVZGQADABSU-RERZDIOCSA-N
SMILESCCC(C)C(NC(=O)C(CCCN=C(N)N)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CCCN=C(N)N)NC(C)=O)C(=O)NC(CCCCN)C(N)=O
Storage condition-20°C

Synonyms

L-Lysinamide, N-acetyl-N-(diaminomethylene)-L-ornithyl-L-tyrosyl-L-tyrosyl-N-(diaminomethylene)-L-ornithyl-L-isoleucyl-
N-acetyl-N-(diaminomethylidene)-L-ornithyl-L-tyrosyl-L-tyrosyl-N-(diaminomethylidene)-L-ornithyl-L-isoleucyl-L-lysinamide
Ac-RYYRIK amide
AC-ARG-TYR-TYR-ARG-ILE-LYS-NH2
N-Acetyl-N-(diaminomethylene)-L-ornithyl-L-tyrosyl-L-tyrosyl-N-(diaminomethylene)-L-ornithyl-L-isoleucyl-L-lysinamide
ACETYL-RYYRIK,AMIDE
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