UFP-101

Pricing Availability Delivery Time Qty
Cat.No. 1552 - UFP-101 | N-(Bn)Gly-Gly-Gly-Phe-Thr-Gly-Ala-Arg-Lys-Ser-Ala-Arg-Lys-Arg-Lys-Asn-Gln-NH2 | CAS No. 849024-68-6
Description: Potent, selective silent antagonist for NOP
Alternative Names: [Nphe1,Arg14,Lys15]Nociceptin-NH2
Datasheet
Citations (2)
Literature

Biological Activity

Potent, selective and competitive silent antagonist for the NOP opioid receptor. Binds to NOP with high affinity (pKi = 10.24) and displays > 3000-fold selectivity over δ, μ and κ opioid receptors. Antinociceptive and opposes the action of nociceptin in vivo.

Technical Data

M. Wt 1908.19
Formula C82H138N32O21
Sequence GGGFTGARKSARKRKNQ

(Modifications: Gly-1 = N-(Bn)Gly, Gln-17 = C-terminal amide)

Storage Desiccate at -20°C
CAS Number 849024-68-6
PubChem ID 16152632
InChI Key DOLKPWDXAQZKNJ-LGCGZHPXSA-N
Smiles C[C@@H](O)[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)CNC(=O)CNC(=O)CNCC1=CC=CC=C1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 1908.19. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.52 mL 2.62 mL 5.24 mL
5 mM 0.1 mL 0.52 mL 1.05 mL
10 mM 0.05 mL 0.26 mL 0.52 mL
50 mM 0.01 mL 0.05 mL 0.1 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Calo et al (2002) [Nphe1,Arg14,Lys15]Nociceptin-NH2, a novel potent and selective antagonist of the nociceptin/orphanin FQ receptor. Br.J.Pharmacol. 136 303 PMID: 12010780

Gavioli et al (2003) Blockade of nociceptin/orphanin FQ-NOP receptor signalling produces antidepressant-like effects: pharmacological and genetic evidences from the mouse forced swimming test. Eur.J.Neurosci. 17 1987 PMID: 12752799

Marti et al (2003) Pharmacological profiles of presynaptic nociceptin/orphanin FQ receptors modulating 5-hydroxytryptamine and noradrenaline release in the rat neocortex. Br.J.Pharmacol. 138 91 PMID: 12522077

McDonald et al (2003) UFP-101, a high affinity antagonist for the nociceptin/orphanin FQ receptor: radioligand and GTPγ35 binding studies. Naunyn Schmiedebergs Arch.Pharmacol. 367 183 PMID: 12595960


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Keywords: Potent selective silent antagonists NOP Nociceptin Receptors ORL1 OP4 Opioid [Nphe1,Arg14,Lys15]Nociceptin-NH2 NOP Receptors

2 Citations for UFP-101

Citations are publications that use Tocris products. Selected citations for UFP-101 include:

Mahmoud et al (2010) Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons. Mol Pharmacol 77 804 PMID: 20159949

Kuzmin et al (2004) Evidence in locomotion test for the functional heterogeneity of ORL-1 receptors. Br J Pharmacol 141 132 PMID: 14662736


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