Helen Frankenthaler Foundation

Dermaseptin CAS 136212-91-4

Dermorphin

Dermorphin

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin.

Description of Dermorphin

Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin.

Dermorphin, a peptide isolated from the skin of Phyllomedusa frogs and the peptide receptor (NOP) component by the endogenous agonist nociceptin/orphanin FQ (N/OFQ). In displacement binding studies at CHOhMu, Dermorphin and DeNo displac the binding of [3H]-DPN in a concentration dependent and saturable manner. Dermorphin displays an affinity of 7.17, while N/OFQ fails to displace [3H]-DPN at the Delta receptor. Dermorphin and DeNo stimulate the binding of GTPγ[35S] in a concentration dependent and saturable manner at the Mu receptor[2].

[1]. Tiwari V, et al. Activation of Peripheral μ-opioid Receptors by Dermorphin [D-Arg2, Lys4] (1-4) Amide Leads to Modality-preferred Inhibition of Neuropathic Pain. Anesthesiology. 2016 Mar;124(3):706-20. [2]. Bird MF, et al. Characterisation of the Novel Mixed Mu-NOP Peptide Ligand Dermorphin-N/OFQ (DeNo). PLoS One. 2016 Jun 7;11(6):e0156897.

Protocol of Dermorphin

Kinase experiment:Membrane protein (40 μg) is incubated in 0.5 mL volume of 50 mM Tris, 0.2 mM EGTA, 1 mM MgCl2, 100 mM NaCl, 0.1% BSA, 0.15 mM bacitracin; pH 7.4, GDP (33 μM), and ∼150 pM GTPγ[35S]. Varying concentrations of reference ligands (Dermorphin, N/OFQ, Dynorphin-A and Leu-enkephalin) or DeNo (1 pM-10 μM) is added prior to incubation. Non-specific binding is determined in the presence of unlabeled GTPγS (10 μM). Samples are incubated at 30°C for 1 h with gentle agitation. Reactions are terminated by vacuum filtration through dry Whatman GF/B filters, using a Brandel harvester[2].

References:

[1]. Tiwari V, et al. Activation of Peripheral μ-opioid Receptors by Dermorphin [D-Arg2, Lys4] (1-4) Amide Leads to Modality-preferred Inhibition of Neuropathic Pain. Anesthesiology. 2016 Mar;124(3):706-20.

[2]. Bird MF, et al. Characterisation of the Novel Mixed Mu-NOP Peptide Ligand Dermorphin-N/OFQ (DeNo). PLoS One. 2016 Jun 7;11(6):e0156897.

Chemical Properties of Dermorphin

Cas No.77614-16-5 SDF

Canonical SMILES Tyr-{d-Ala}-Phe-Gly-Tyr-Pro-Ser-NH2

Formula C 40 H 50 N 8 O 10 M.Wt 802.87

Solubility H 2 O : 120 mg/mL (149.46 mM; Need ultrasonic)Storage Store at -20°C

General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.

To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.

Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Dermorphin

Prepare stock solution

1 mg 5 mg 10 mg

1 mM 1.2455 mL 6.2277 mL 12.4553 mL

5 mM 249.1 μL 1.2455 mL 2.4911 mL

10 mM 124.6 μL 622.8 μL 1.2455 mL

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Chemical Structure

Molecular weight g/mol

Enter a commonly used written chemical formula, such as:Na2SO4、 Fe3[Fe(CN)6]2 、 Fe3(Fe(CN)6)2

A simple formula also allows:CH2=C(CH3)2、H3C-(CH2)7-CH=CH-(CH2)7-COOH.

In vivo Formulation Calculator (Clear solution) of Dermorphin