(D-Arg¹,D-Phe⁵,D-Trp⁷·⁹,Leu¹¹)-Substance P

H-D-Arg-Pro-Lys-Pro-D-Phe-Gln-D-Trp-Phe-D-Trp-Leu-Leu-NH₂

Product Number: 4013823

CAS Number: 96736-12-8

€ 71.70 – € 285.70

Custom/Bulk Quote

Pack size available	1mg, 5mg

Please select pack size:

Pack size available

Clear

Add to your inquiry

Product Description

(D-Arg¹,D-Phe⁵,D-Trp⁷·⁹,Leu¹¹)-Substance P initially described as a low potency ghrelin receptor antagonist has surprisingly been found to be a full inverse agonist (EC₅₀ = 5.2 nM). In COS-7 cells transiently transfected with the ghrelin receptor the substance P analog rPKPfQwFwLL decreased the constitutive signaling down to levels observed in untransfected cells. Assuming that constitutive signaling of the ghrelin receptor is of physiological relevance in the regulation of appetite control, inverse agonists of the ghrelin receptor could be interesting for the treatment of obesity. So, Asakawa et al. found that peripherally administered H-6395 decreased food intake in lean mice, in mice with diet induced obesity, and in ob/ob obese mice.

ADS

ADS lookup

MSDS

MSDS lookup

Diabetes Peptides

Novel linear antagonists of the antidiuretic (V2) and vasopressor (V1) responses to vasopressin.

M.Manning et al., Int. J. Pept. Protein Res., 32, 455 (1988)

Antagonism of ghrelin receptor reduces food intake and body weight gain in mice.

A.Asakawa et al., Gut, 52, 947 (2003)

[D-Arg1,D-Phe5,D-Trp7,9,Leu11]substance P, a potent bombesin antagonist in murine Swiss 3T3 cells, inhibits the growth of human small cell lung cancer cells in vitro.

P.J.Woll and E.Rozengurt, Proc. Natl. Acad. Sci. USA, 85, 1859 (1988)

Block of the hyoscine-resistant opiate withdrawal contracture of ileum by a new substance P antagonist [D-Arg1,D-Phe5,D- Trp7,9,Leu 11]substance P.

K.Tsou et al., Eur. J. Pharmacol., 110, 155 (1985)

[D-Arg1, D-Phe5, D-Trp7,9, Leu11] substance P induces apoptosis in lung cancer cell lines in vitro.

J.G.Reeve and N.M.Bleehen, Biochem. Biophys. Res. Commun., 199, 1313 (1994)

Metabolism of the anticancer peptide H-Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2.

D.A.Jones et al., Peptides, 16, 777 (1995)

Unexpected effects of peptide and nonpeptide substance P receptor antagonists on basal prolactin and growth hormone release in vitro.

P.Heinz-Erian et al., Gastroenterology, 90, 1455 (1986)

High constitutive signaling of the ghrelin receptor--identification of a potent inverse agonist.

H.Houben and C.Denef, Peptides, 14, 109 (1993)

B.Holst et al., Mol. Endocrinol., 17, 2201 (2003)

Molecular weight: 1516.86

Chemical Formula: C₇₉H₁₀₉N₁₉O₁₂

Storage Temperature: < -15°C

Synonyms: [DArg1, DPhe5, DTrp7,9, Leu11] Substance P

One Letter code: rPKPfQwFwLL-NH₂

Source: Synthetic

Old Product Number: H-6935

Country

Inquiry List