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

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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 full inverse agonist and antagonist at other neuropeptide receptors; anticancer in vitro
Datasheet
Citations (3)
Literature

Biological Activity

Broad spectrum neuropeptide antagonist/inverse agonist. 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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 1 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 1516.85. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.66 mL 3.3 mL 6.59 mL
5 mM 0.13 mL 0.66 mL 1.32 mL
10 mM 0.07 mL 0.33 mL 0.66 mL
50 mM 0.01 mL 0.07 mL 0.13 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P, please let us know.

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Keywords: [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, Ghrelin, Receptors, Other, Tachykinin, Ghrelin, Receptors, 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 growth hormone 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


Do you know of a great paper that uses [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-Substance P from Tocris? If so please let us know.

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