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Submit Review[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P is a broad spectrum neuropeptide inverse agonist and antagonist. Potent full inverse agonist for the ghrelin receptor (EC50 = 5.2 nM); diminishes constitutive ghrelin receptor signaling. Also antagonist at tachykinin, bradykinin, CCK and bombesin receptors. Induces apoptosis and inhibits cancer cell growth in vitro.
分子量 | 1516.85 |
公式 | C79H109N19O12 |
序列 |
RPKPFQWFWLL (Modifications: Arg-1 = D-Arg, Phe-5 = D-Phe, Trp-7 = Trp-9 = D-Trp, Leu-11 = C-terminal amide) |
储存 | Desiccate at -20°C |
CAS Number | 96736-12-8 |
PubChem ID | 25091011 |
InChI Key | XVOCEQLNJQGCQG-ACRSGXKRSA-N |
Smiles | [H]N[C@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1=CC=CC=C1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Holst et al (2003) High constitutive signaling of the ghrelin receptor - identification of a potent inverse agonist. Mol.Endocrinol. 17 2201 PMID: 12907757
Jarpe et al (1998) [D-Arg1, D-Phe5, D-Trp7,9, Leu11] Substance P acts as a biased agonist toward neuropeptide and chemokine receptors. J.Biol.Chem. 273 3097 PMID: 9446627
Reeve and Bleehen (1994) [D-Arg1, D-Phe5, D-Trp7,9, Leu11] Substance P induces apoptosis in lung cancer cells in vitro. Biochem.Biophys.Res.Commun. 199 1313 PMID: 7511895
关键词: [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P supplier, Substance, P, broad, spectrum, neuropeptide, receptor, antagonists, inverse, agonists, Potent, ghrelin, Tachykinin, Neurokinin, Receptors, GHS-R1a, Growth, Hormone, Secretagog, Receptor, 1a, Ghrelin, [D-Arg1D-Phe5D-Trp79Leu11]-SubstanceP, neuropeptides, Other, 1946, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P 的部分引用包括:
Torres-Fuentes et al (2014) Devil's Claw to suppress appetite--ghrelin receptor modulation potential of a Harpagophytum procumbens root extract. Oncotarget 9 e103118 PMID: 25068823
Schellekens et al (2013) Promiscuous dimerization of the GH secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling. J Biol Chem 288 181 PMID: 23161547
Pastor-Cavada et al (2016) A novel non-peptidic agonist of the ghrelin receptor with orexigenic activity In vivo Scientific Reports 6 36456 PMID: 27819353
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.