Antagonist G TFA

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.

Product information

Molecular Weight: 1065.21

Formula: C51H67F3N12O8S

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

Smiles: CC(C)C[C@H](NC(=O)[C@@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@H](CC1=CC=CC=C1)N(C)C(=O)[C@@H](CC1=CNC2=CC=CC=C12)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CCSC)C(N)=O.OC(=O)C(F)(F)F

InChiKey: GUDATFWCKFMCTO-RGVCNNQFSA-N

InChi: InChI=1S/C49H66N12O6S.C2HF3O2/c1-29(2)23-39(45(64)57-38(43(51)62)20-22-68-4)58-46(65)40(25-31-27-55-36-18-10-8-15-33(31)36)59-47(66)42(24-30-13-6-5-7-14-30)61(3)48(67)41(26-32-28-56-37-19-11-9-16-34(32)37)60-44(63)35(50)17-12-21-54-49(52)53;3-2(4,5)1(6)7/h5-11,13-16,18-19,27-29,35,38-42,55-56H,12,17,20-26,50H2,1-4H3,(H2,51,62)(H,57,64)(H,58,65)(H,59,66)(H,60,63)(H4,52,53,54);(H,6,7)/t35-,38-,39-,40+,41+,42-;/m0./s1

Technical Data

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

In Vitro:

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%.

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.

Products are for research use only. Not for human use.