S86987 |
2-ADAMANTANECARBONYL-ARG-PHE-NH2 |
源叶(MedMol) | 98% |
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- 产品描述: RF9 is a potent and selective Neuropeptide FF receptor antagonist, with Ki values of 58 and 75 nM for hNPFF1R and hNPFF2R, respectively
- 靶点: hNPFF1R:58 nM (Ki);hNPFF2R:75 nM (Ki);NeuropeptideYReceptor
- 体内研究:
RF9 (0.1 mg/kg, s.c. ) with heroin coadministration prevents heroin-induced delayed hyperalgesia and tolerance. RF9 (10 μg) infused alone does not result in a significant alteration of MAP or heart rate. Conversely, MAP and heart rate increases evoked by NPFF are significantly blocked when NPFF is applied in conjunction with RF9. Animal Model: Rats. Dosage: 0.1 mg/kg. Administration: S.C. 30 min before 0.3 mg/kg heroin or saline on basal nociceptive threshold in rats. Result: Opposed to delaye heroin-induced hyperalgesia and associated tolerance.
- 参考文献:
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. 2. Ting Zhang, et al. Discovery of Two Novel Branched Peptidomimetics Containing endomorphin-2 and RF9 Pharmacophores: Synthesis and Neuropharmacological Evaluation. Bioorg Med Chem. 2019 Feb 15;27(4):630-643.
- 溶解性: Soluble in DMSO、H2O
- 保存条件: 2-8℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 1.676 ml 8.38 ml 16.76 ml 5 mM 0.335 ml 1.676 ml 3.352 ml 10 mM 0.168 ml 0.838 ml 1.676 ml 50 mM 0.034 ml 0.168 ml 0.335 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)