Antagonist G TFA 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.
Molecular Weight: 1065.21
Chemical Name: (S)-N-((5S, 8S, 11R, 14S, 17R)-11-((1H-indol-3-yl)methyl)-14-benzyl-5-carbamoyl-18-(1H-indol-3-yl)-8-isobutyl-15-methyl-7, 10, 13, 16-tetraoxo-2-thia-6, 9, 12, 15-tetraazaoctadecan-17-yl)-2-amino-5-(diaminomethyleneamino)pentanamide 2, 2, 2-trifluoroacetate
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
Antagonist G (0-100 μM) induces apoptosis is redox-sensitive and caspase-dependently in SCLC cells. Antagonist G activates JNK1 in SCLC cells. 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%.
- 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.
- 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.
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