标签归档：拮抗剂

Antagonist G

发表于由

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Antagonist G  纯度: 95.0%

Antagonist G 是有效的后叶加压素 (vasopressin) 的拮抗剂。Antagonist G 也是弱的 GRP 和缓激肽的弱拮抗剂。Antagonist G 可诱导 AG-1 的转录，是癌细胞对化疗增敏。

Antagonist G

Antagonist G Chemical Structure

CAS No. : 115150-59-9

规格 价格 是否有货 数量
1 mg ￥1500 In-stock
5 mg ￥4500 In-stock
10 mg   询价  
50 mg   询价  

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生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

951.19

Formula

C49H66N12O6S
CAS 号

115150-59-9
Sequence Shortening

RW-{Me-Phe}-WLM-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Protect from light

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro: 

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.
参考文献

  • [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.

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