Dermorphin Analog 是 Dermorphin 的类似物。Dermorphin 为两栖类皮肤中发现的天然七肽,为 μ-阿片受体 (μ-opioid receptor) 激动剂。
Dermorphin Analog Chemical Structure
规格
价格
是否有货
1 mg
¥900
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5 mg
¥1800
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10 mg
¥2800
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生物活性
Dermorphin Analog is an analog of Dermorphin. Dermorphin is a natural heptapeptide μ-opioid receptor agonist found in amphibian skin.
分子量
901.43
Formula
C44H59N11O10
Sequence
Tyr-{d-Arg}-Phe-{SAR}-Tyr-Pro-Ser-NH2
Sequence Shortening
Y-{d-Arg}-F-{SAR}-YPS-NH2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;
H2O
Peptide Solubility and Storage Guidelines:
1.;;Calculate the length of the peptide.
2.;;Calculate the overall charge of the entire peptide according to the following table:
;
Contents
Assign value
Acidic amino acid
Asp (D), Glu (E), and the C-terminal -COOH.
-1
Basic amino acid
Arg (R), Lys (K), His (H), and the N-terminal -NH2
+1
Neutral amino acid
Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q)
0
3.;;Recommended solution:
Overall charge of peptide
Details
Negative (lt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, add NH4OH (lt;50 μL). 3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0)
1.;;Try to dissolve the peptide in water first. 2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0)
1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Inhibition of neuropathic pain[1].
IC50 Target
μ-opioid receptor (MOR)[1]
体外研究 (In Vitro)
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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
802.87
Formula
C40H50N8O10
CAS 号
77614-16-5
Sequence
Tyr-{d-Ala}-Phe-Gly-Tyr-Pro-Ser-NH2
Sequence Shortening
Y-{d-Ala}-FGYPS-NH2
中文名称
皮啡肽
运输条件
Room temperature in continental US; may vary elsewhere.
[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.
Kinase Assay [2]
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].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献
[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.