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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGinsenoside RfCat. No.: HY-N0601CAS No.: 52286-58-5Synonyms: Panaxoside Rf分式: CHO分量: 801.01作靶点: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-2
2、0C 1 month溶解性数据体外实验 Ethanol : 50 mg/mL (62.42 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.2484 mL 6.2421 mL 12.4842 mL5 mM 0.2497 mL 1.2484 mL 2.4968 mL10 mM 0.1248 mL 0.6242 mL 1.2484 mL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,并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,
3、再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.12 mM); Clear solution2. 请依序添加每种溶剂: 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.12 mM); Clear solution3. 请依序添加每种溶剂:
4、10% EtOH 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (3.12 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ginsenoside Rf参根的种微量成分。 Ginsenoside Rf 抑制 N 型 Ca2+ 通道。IC50 & Target N-Type Ca2+ Channel体外研究 Ginsenoside Rf is a saponin, which is present in only trace amounts
5、within ginseng. At saturatingconcentrations, Ginsenoside Rf rapidly and reversibly inhibits N-type, and other high-threshold, Ca2+channels in rat sensory neurons to the same degree as a maximal dose of opioids. The effect is dose-dependent (half-maximal inhibition: 40 M) and it is virtually eliminat
6、ed by pretreatment of the neurons withpertussis toxin, an inhibitor of G(o) and Gi GTP-binding proteins. Ginsenoside Rf also inhibits Ca2+ channelsin the hybrid F-11 cell line 1.体内研究 Since inhibition of Ca2+ channels in sensory neurons contributes to antinociception by opioids, analgesicactions of G
7、insenoside Rf are tested. Dose-dependent antinociception is found by systemic administration ofGinsenoside Rf in mice using two separate assays of tonic pain: in the acetic acid abdominal constrictiontest, the ED50 is 569 mg/kg, a concentration similar to those reported for aspirin and acetaminophen
8、 in thesame assay; in the tonic phase of the biphasic formalin test, the ED50 is 12932 mg/kg 2.PROTOCOLAnimal Mice 2Administration 2 Naive, adult (7-12 week old) mice of outbred Swiss-Webster stock are used in all in vivo experiments. Miceare brought to a quiet testing room, and acclimated to table-
9、top Plexiglas observation chambers (30 cm high;30 cm diameter) for 30 min. They are then weighed and injected with Ginsenoside Rf (25, 50, or 75 mg/kg) orvehicle (preceded by naloxone or saline in one experiment). Twenty min later, a 0.9% solution of glacialacetic acid is injected intraperitoneally
10、(i.p.) in a volume of 10 mL/kg. For the next 30 min, the number ofconstrictions (writhes)-strong contractions of the abdominal musculature accompanied by dorsoflexion of theback and extension of the hindlimbs-are counted and recorded in 5-min blocks. Four mice (one per chamber)are observed simultane
11、ously by a single, experienced experimenter. To control for the considerable circadianand other environmental variance accompanying this nociceptive assay, two vehicle controls are testedalongside two Ginsenoside Rf-administered mice in every experimental session 2.MCE has not independently confirme
12、d the accuracy of these methods. They are for reference only.REFERENCES1. Nah SY, et al. A trace component of ginseng that inhibits Ca2+ channels through a pertussis toxin-sensitive G protein. Proc Natl Acad SciU S A. 1995 Sep 12;92(19):8739-43.2. Mogil JS, et al. Ginsenoside Rf, a trace component of ginseng root, produces antinociception in mice. Brain Res. 1998 May11;792(2):218-28.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMcePdfHeightCau
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