Home / Pharmacology / GPCRs / 7-TM Receptors / Peptide Receptors / Ghrelin Receptors / Ghrelin Receptor Inverse Agonists / [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P

Cat. No. 1946 3 Citations Submit a Review Datasheet / COA / SDS

Discontinued Product

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P (Cat. No. 1946) has been withdrawn from sale for commercial reasons.
Cat.No. 1946 - [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P | D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH2 | CAS No. 96736-12-8
Description: Potent ghrelin receptor inverse agonist; Antagonist at other neuropeptide receptors
Datasheet
Citations (3)
Reviews
Literature (3)
Biological Activity Technical Data Datasheets References

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.

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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:

Schellekens et al (2013) Promiscuous dimerization of the GH secretagogue receptor (GHS-R1a) attenuates ghrelin-mediated signaling. J Biol Chem 288 181 PMID: 23161547

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

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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