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.
For research use only. We do not sell to patients.
- Formula: C51H67F3N12O8S
- Molecular Weight:1065.21
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Vasopressin Receptor Isoforms
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Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SCLC cell lines NCI-H69, NCI-H510 and CHO-K1 cells.
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Concentration:0-100 μM.
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Incubation Time:24 h.
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Result:Inhibited cell growh.
Chemical Information
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Molecular Weight 1065.21
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Formula C51H67F3N12O8S
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Sequence Shortening
RW-{Me-Phe}-WLM-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent & Solubility
H2O
Peptide Solubility and Storage Guidelines:
1. Calculate the length of the peptide.
2. Calculate the overall charge of the entire peptide according to the following table:
| Contents | Assign value | |
| Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 |
| Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 |
| Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution:
| Overall charge of peptide | Details |
| Negative (<0) |
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
| Positive (>0) |
1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
| Zero (=0) |
1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)