RF 9
目录号 : GC15469
An NPFF receptor antagonist
Cas No.:876310-60-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Rats: Rats (n=5) are catheterized for measurement of arterial blood pressure and receive an in-dwelling cannula into the lateral cerebral ventricle. Arterial blood pressure and heart rate are continuously monitored. NPFF (10 μg in 10 μL of saline) is injected into the lateral ventricle over 15 to 20 sec. Control injections of saline (10 μL) are carried out in the same animals. Upon return of blood pressure to baseline, RF9 (10 μg) is injected i.c.v., followed by another i.c.v. injection of NPFF with RF9. After 1.5 h., another i.c.v. infusion of NPFF is repeated[1]. |
References: [1]. Simonin F, et al. RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia. Proc Natl Acad Sci U S A. 2006 Jan 10;103(2):466-71. | |
Ki: 58 nM for NPFF1; 75 nM for NPFF2
RF 9 is a neuropeptide FF receptors antagonist.
Neuropeptide FF (NPFF) has been isolated originally from bovine brain through its cross-reaction with antibodies to the molluscan cardioexcitory peptide FMRF-NH2, which possesses the similar C-terminal sequence. Recent studies shows that NPFF belongs to a neuropeptide family including two G protein-coupled receptors (NPFF1 and NPFF2) and two precursors (pro-NPFFA and pro-NPFFB). Both in vitro and in vivo studies have indicated that NPFF involves in a variety of biological actions.
In vitro: RF9 was found as a potent and selective NPFF receptor antagonist. RF9 was shown to be able to selectively bind to recombinant NPFF1 or NPFF2 receptors expressed in CHO or COS-1 cell and could also in vitro antagonize the agonism induced by NPFF and NPVF in the functional assays [1].
In vivo: Aminal in vivo study showed RF9 (30 nmol) injection failed to induce significant effect, but RF9 could completely antagonize the hypothermia of NPFF after cerebral administration in mice. Additionally, RF9 (30 nmol) co-injected in the third ventricle reduced the hypothermia induced by morphine or nociceptin/orphanin [2].
Clinical trial:N/A
References:
[1] Fang Q,Wang YQ,He F,Guo J,Guo J,Chen Q,Wang R. Inhibition of neuropeptide FF (NPFF)-induced hypothermia and anti-morphine analgesia by RF9, a new selective NPFF receptors antagonist. Regul Pept.2008 Apr 10;147(1-3):45-51.
[2] Wang YQ,Guo J,Wang SB,Fang Q,He F,Wang R. Neuropeptide FF receptors antagonist, RF9, attenuates opioid-evoked hypothermia in mice. Peptides.2008 Jul;29(7):1183-90.
| Cas No. | 876310-60-0 | SDF | |
| 化学名 | (3S,5S,7S,Z)-N-((S,Z)-5-guanidino-1-hydroxy-1-(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)pentan-2-yl)adamantane-1-carbimidic acid | ||
| Canonical SMILES | N=C(O)[C@](/N=C(O)/[C@](/N=C(O)/C12C[C@@]3([H])C[C@](C1)([H])C[C@](C2)([H])C3)([H])CCCNC(N)=N)([H])CC4=CC=CC=C4 | ||
| 分子式 | C26H38N6O3 | 分子量 | 482.62 |
| 溶解度 | DMSO: 5 mg/ml,Water: 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 | 2.072 mL | 10.3601 mL | 20.7202 mL |
| 5 mM | 0.4144 mL | 2.072 mL | 4.144 mL |
| 10 mM | 0.2072 mL | 1.036 mL | 2.072 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。
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