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Dermorphin Sale

(Synonyms: 皮啡肽) 目录号 : GC31168

An opioid peptide

Dermorphin Chemical Structure

Cas No.:77614-16-5

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10mm*1mlinwater
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1mg
¥360.00
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5mg
¥720.00
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10mg
¥1,152.00
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25mg
¥1,843.00
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50mg
¥2,592.00
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Sample solution is provided at 25 µL, 10mM.

Description

Dermorphin is an opioid peptide originally isolated from the skin of South American frogs (Ph. sauvagei).1 It binds to μ-opioid receptors (Ki = 0.54 nM) and is selective for μ- over δ-opioid receptors in radioligand binding assays (Ki = 929 nM). In vivo, dermorphin (1.9 ?mol/kg, i.p.) inhibits noxious stimuli-induced neuronal firing in the nucleus lateralis anterior and ventrobasal complex in rats.2 It inhibits the electrical stimulation-induced C fiber response in rat dorsal horn nociceptive neurons. Dermorphin (10-120 pmol/animal, i.c.v.) delays gastric emptying, inhibits gastric acid secretion, and slows colonic motility in pylorus-ligated rats.

1.Usenko, A.B., Emel'yanova, T.G., and MIasoedov, N.F.Dermorphins are natural opioids with an unique primary structure that determines their biological specificityBiol. Bull. Russ. Acad. Sci.29154-164(2002) 2.Melchiorri, P., and Negri, L.The dermorphin peptide familyGen. Pharmacol.27(7)1099-1107(1996)

实验参考方法

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.

化学性质

Cas No. 77614-16-5 SDF
别名 皮啡肽
Canonical SMILES Tyr-{d-Ala}-Phe-Gly-Tyr-Pro-Ser-NH2
分子式 C40H50N8O10 分子量 802.87
溶解度 H2O : 120 mg/mL (149.46 mM; Need ultrasonic) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.2455 mL 6.2277 mL 12.4553 mL
5 mM 0.2491 mL 1.2455 mL 2.4911 mL
10 mM 0.1246 mL 0.6228 mL 1.2455 mL
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