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Submit Review[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
Description: Potent ghrelin receptor inverse agonist; Antagonist at other neuropeptide receptors
Biological Activity
[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.
Technical Data
| M. Wt | 1516.85 |
| Formula | C79H109N19O12 |
| Sequence |
RPKPFQWFWLL (Modifications: Arg-1 = D-Arg, Phe-5 = D-Phe, Trp-7 = Trp-9 = D-Trp, Leu-11 = C-terminal amide) |
| Storage | 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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets
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References
References are publications that support the biological activity of the product.
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
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Keywords: [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
3 Citations for [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P
Citations are publications that use Tocris products. Selected citations for [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P include:
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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Literature in this Area
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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Peptides Involved in Appetite Modulation Scientific Review
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.