Antagonist G (trifluoroacetate salt)
(Synonyms: Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2, Arg6,D-Trp7,9,NmePhe8-substance P (6-11)) 目录号 : GC49259
A neuropeptide antagonist
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Antagonist G is a neuropeptide antagonist.1,2,3 It inhibits the binding of vasopressin to rat liver or Swiss 3T3 membranes (IC50s = 3.5 and 2.2 µM, respectively) and vasopressin-induced production of inositol phosphate in Swiss 3T3 fibroblasts (IC50 = 1 µM).1 Antagonist G (50 µM) induces apoptosis and the production of reactive oxygen species (ROS) in NCI H69 small cell lung cancer (SCLC) cells.2 It reduces tumor growth in an NCI H69 mouse xenograft model when administered at a dose of 45 µg/g.3
1.Seckl, M.J., Newman, R.H., Freemont, P.S., et al.Substance P-related antagonists inhibit vasopressin and bombesin but not 5’-3-O-(thio)triphosphate-stimulated inositol phosphate production in swiss 3T3 cellsJ. Cell Physiol.163(1)87-95(1995) 2.MacKinnon, A.C., Waters, C., Rahman, I., et al.[Arg6, D-Trp7,9, NmePhe8]-substance P (6-11) (antagonist G) induces AP-1 transcription and sensitizes cells to chemotherapyBr. J. Cancer.83(7)941-948(2000) 3.Langdon, S., Sethi, T., Ritchie, A., et al.Broad spectrum neuropeptide antagonists inhibit the growth of small cell lung cancer in vivoCancer Res.52(16)4554-4557(1992)
| Cas No. | N/A | SDF | |
| 别名 | Arg-D-Trp-NmePhe-D-Trp-Leu-Met-NH2, Arg6,D-Trp7,9,NmePhe8-substance P (6-11) | ||
| Canonical SMILES | CSCC[C@@H](C(N)=O)NC([C@H](CC(C)C)NC([C@@H](CC1=CNC2=CC=CC=C12)NC([C@H](CC3=CC=CC=C3)N(C)C([C@H](NC([C@@H](N)CCCNC(N)=N)=O)CC4=CNC5=CC=CC=C45)=O)=O)=O)=O.OC(C(F)(F)F)=O | ||
| 分子式 | C49H66N12O6S·XCF3COOH | 分子量 | 951.2 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 20 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0513 mL | 5.2565 mL | 10.513 mL |
| 5 mM | 0.2103 mL | 1.0513 mL | 2.1026 mL |
| 10 mM | 0.1051 mL | 0.5257 mL | 1.0513 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
RF9 excitation of GnRH neurons is dependent upon Kiss1r in the adult male and female mouse
Endocrinology 2014 Dec;155(12):4915-24.PMID:25322463DOI:10.1210/en.2014-1517
The neuropeptide FF receptor antagonist 1-adamantanecarbonyl-Arg-Phe-NH2 trifluoroacetate salt (RF9) has been found to be a remarkably potent activator of gonadotropin secretion in mammals. However, the mechanism of RF9 action on the reproductive axis is unknown. Using acute brain slice electrophysiology in genetically modified mouse models, we have investigated the possibility that RF9 may activate GnRH neurons. In transgenic GnRH-GFP male and female mice, RF9 was found to exert potent, dose-dependent, stimulatory effects on the firing rate of approximately 70% of GnRH neurons. These effects occurred directly on GnRH neurons and were independent of fast amino acid transmission. To assess RF9's action as an neuropeptide FF receptor antagonist at the GnRH neuron, its ability to antagonize the inhibitory effects of RFamide-related peptide-3 on GnRH neuron firing was examined. RF9 exhibited variable ability to prevent the inhibitory effects of RFamide-related peptide-3 on GnRH neurons. Whole-cell recordings from GnRH neurons showed that RF9 generated an inward current in GnRH neurons reminiscent of that evoked by kisspeptin. We therefore examined RF9 actions in kisspeptin receptor knockout mice. RF9 was found to have no effects at all on GnRH neurons in GnRH-GFP;Kiss1r-null mice, although these cells exhibited normal intrinsic electrical properties and remained responsive to GABA and glutamate. This study reveals that RF9 directly activates GnRH neurons in the mouse and that this is dependent upon Kiss1r expression.