[Orn5]-URP

Urotensin-II (UT) receptor antagonist CAS# 782485-03-4

[Orn5]-URP

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Chemical structure

[Orn5]-URP

3D structure

Chemical Properties of [Orn5]-URP

Cas No. 782485-03-4 SDF Download SDF
PubChem ID 134812802 Appearance Powder
Formula C48H62N10O10S2 M.Wt 1003.2
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 1 mg/ml in water
Sequence ACFWXYCV

(Modifications: X = Orn, Disulfide bridge between 2 - 7)

Chemical Name (2S)-2-[[(4R,10S,13S)-19-[[(2S)-2-aminopropanoyl]amino]-10-(3-aminopropyl)-16-benzyl-7-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]amino]-3-methylbutanoic acid
SMILES CC(C)C(C(=O)O)NC(=O)C1CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CC2=CC=C(C=C2)O)CCCN)CC3=CNC4=CC=CC=C43)CC5=CC=CC=C5)NC(=O)C(C)N
Standard InChIKey BPLKRLYKWHXTMO-PDWAYWLXSA-N
Standard InChI InChI=1S/C48H62N10O10S2/c1-26(2)40(48(67)68)58-47(66)39-25-70-69-24-38(56-41(60)27(3)50)46(65)54-35(20-28-10-5-4-6-11-28)43(62)55-37(22-30-23-51-33-13-8-7-12-32(30)33)45(64)52-34(14-9-19-49)42(61)53-36(44(63)57-39)21-29-15-17-31(59)18-16-29/h4-8,10-13,15-18,23,26-27,34-40,51,59H,9,14,19-22,24-25,49-50H2,1-3H3,(H,52,64)(H,53,61)(H,54,65)(H,55,62)(H,56,60)(H,57,63)(H,58,66)(H,67,68)/t27-,34-,35?,36?,37-,38?,39-,40-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of [Orn5]-URP

DescriptionUrotensin-II (UT) receptor pure antagonist (pEC50 = 7.24). Displays no agonist activity unlike other U-II/URP analogs. Inhibits the action of U-II in the rat aorta ring assay.

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References on [Orn5]-URP

[Orn5]URP acts as a pure antagonist of urotensinergic receptors in rat cortical astrocytes.[Pubmed:18082287]

Peptides. 2008 May;29(5):813-9.

Cultured rat astrocytes, which express functional urotensin II (UII)/UII-related peptide (URP) receptors (UT), represent a very suitable model to investigate the pharmacological profile of UII and URP analogs towards native UT. We have recently designed three URP analogs [D-Trp4]URP, [Orn5]URP and [D-Tyr6]URP, that act as UT antagonists in the rat aortic ring bioassay. However, it has been previously reported that UII/URP analogs capable of inhibiting the contractile activity of UII possess agonistic activity on UT-transfected cells. In the present study, we have compared the ability of URP analogs to compete for [125 I]URP binding and to modulate cytosolic calcium concentration ([Ca2+]c) in cultured rat astrocytes. All three analogs displaced radioligand binding: [D-Trp4]URP and [D-Tyr6]URP interacted with high- and low-affinity sites whereas [Orn5]URP only bound high-affinity sites. [D-Trp4]URP and [D-Tyr6]URP both induced a robust increase in [Ca2+]c in astrocytes while [Orn5]URP was totally devoid of activity. [Orn5]URP provoked a concentration-dependent inhibition of URP- and UII-evoked [Ca2+]c increase and a rightward shift of the URP and UII dose-response curves. The present data indicate that [D-Trp4]URP and [D-Tyr6]URP, which act as UII antagonists in the rat aortic ring assay, behave as agonists in the [Ca2+]c mobilization assay in cultured astrocytes, whereas [Orn5]URP is a pure selective antagonist in both rat aortic ring contraction and astrocyte [Ca2+]c mobilization assays.

Structure-activity relationships and structural conformation of a novel urotensin II-related peptide.[Pubmed:15476952]

Peptides. 2004 Oct;25(10):1819-30.

Urotensin II (UII) has been described as the most potent vasoconstrictor peptide and recognized as the endogenous ligand of the orphan G protein-coupled receptor GPR14. Recently, a UII-related peptide (URP) has been isolated from the rat brain and its sequence has been established as H-Ala-Cys-Phe-Trp-Lys-Tyr-Cys-Val-OH. In order to study the structure-function relationships of URP, we have synthesized a series of URP analogs and measured their binding affinity on hGPR14-transfected cells and their contractile activity in a rat aortic ring bioassay. Alanine substitution of each residue of URP significantly reduced the binding affinity and the contractile activity of the peptides, except for the Ala8-substituted analog that retained biological activity. Most importantly, D-scan of URP revealed that [D-Trp4]URP abrogated and [D-Tyr6]URP partially suppressed the UII-evoked contractile response. [Orn5]URP, which had very low agonistic efficacy, was the most potent antagonist in this series. The solution structure of URP has been determined by 1H NMR spectroscopy and molecular dynamics. URP exhibited a single conformation characterized by an inverse gamma-turn comprising residues Trp-Lys-Tyr which plays a crucial role in the biological activity of URP. These pharmacological and structural data should prove useful for the rational design of non-peptide ligands as potential GPR14 agonists and antagonists.

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