(Arg6,D-Trp7.9,N-Me-Phe8)-Substance P (6-11)

Names

[ Name ]:
(Arg6,D-Trp7.9,N-Me-Phe8)-Substance P (6-11)

[Synonym ]:
arginyl-tryptophyl-n-methylphenylalanyl-tryptophyl-leucyl-methioninamide
AntagonistG,Arg-D-Trp-N-Methyl-Phe-D-Trp-Leu-Met-NH2
ARG-D-TRP-N-ME-PHE-D-TRP-LEU-MET-NH2
H-ARG-D-TRP-N-ME-PHE-D-TRP-LEU-MET-NH2

Biological Activity

[Description]:

Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Vasopressin Receptor

[In Vitro]

Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells[2]. Antagonist G activates JNK1 in SCLC cells[2]. Antagonist G is not intrinsically a free radical oxygen donor but stimulates free radical generation specifically within SCLC cells (6.2-fold) and increases the activity of the redox-sensitive transcription factor AP-1 by 61%[2]. Cell Viability Assay[2] Cell Line: SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells. Concentration: 0-100 μM. Incubation Time: 24 h. Result: Inhibited cell growh.

[References]

[1]. P J Woll, et al. A neuropeptide antagonist that inhibits the growth of small cell lung cancer in vitro. Cancer Res. 1990 Jul 1;50(13):3968-73.

[2]. A C MacKinnon, et al. [Arg6, D-Trp7,9, NmePhe8]-substance P (6–11) (antagonist G) inducesP-1 transcription and sensitizes cells to chemotherapy. Br J Cancer. 2000 Oct; 83(7): 941–948.

Chemical & Physical Properties

[ Density]:
1.35g/cm3

[ Molecular Formula ]:
C₄₉H₆₆N₁₂O₆S

[ Molecular Weight ]:
951.19000

[ Exact Mass ]:
950.49500

[ PSA ]:
324.60000

[ LogP ]:
6.47350

[ Index of Refraction ]:
1.666

Related Compounds

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