Koumine - Alkaloid - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKoumineCat. No.: HY-N1440CAS No.: 1358-76-5分式: CHNO分量: 306.4作靶點: Others作通路: Others儲存式: 4C, sealed storage, away from moisture and light* In solvent : -80C, 6 months; -20C, 1 month (sealedstorage, away from moisture and light)溶解性

2、數(shù)據(jù)體外實驗 DMSO : 31.25 mg/mL (101.99 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.2637 mL 16.3185 mL 32.6371 mL5 mM 0.6527 mL 3.2637 mL 6.5274 mL10 mM 0.3264 mL 1.6319 mL 3.2637 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為

3、保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.79 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (6.79 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO

4、 90% corn oilSolubility: 2.08 mg/mL (6.79 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Koumine從鉤吻 (Gelsemium elegans) 中得到的物堿，具有效抗腫瘤活性，在腫瘤細(xì)胞中能夠增加Bax/Bcl-2 的蛋例和 caspase-3 的表達(dá) 1。Koumine 具有抗焦慮、抗應(yīng)激、抗銀屑病和鎮(zhèn)痛活性 3。在類風(fēng)濕性關(guān)節(jié)炎動物模型中，Koumine 能夠預(yù)防關(guān)節(jié)炎的發(fā)展 2。體外研究 Koumine (

5、0.5, 1 and 2 mg/mL) dose- and time-dependently inhibits the proliferation of MCF-7 cells, with anIC50 of 124 g/mL at 72 h. Koumine induces apoptosis, causes cell cycle arrest at G2/M phase 1.Koumine (0.5, 1 and 2 mg/mL) up-regulates the Bax/Bcl-2 ratio and caspase-3 expression in a dose-dependent ma

6、nner in MCF-7 Cells 1.Koumine (25, 50, 100, and 200M) decreases the protein and mRNA levels of microglia M1 polarizationfactors in LPS-induced BV2 cells 3.體內(nèi)研究 Koumine is less toxic, with the median lethal dose (LD50) of 300.0 mg/kg on Wistar rats. Koumine (0.6, 3, or15 mg/kg/per, p.o.) exhibits ant

7、irheumatic properties in rats with adjuvant-induced arthritis (AIA) andcollagen-induced arthritis (CIA) 2.Koumine inhibits the increase in cytokines in joint tissue and TNF- level in serum at 15 mg/kg, andsuppresses the increase in the serum level of IL-1 at 3 and 15 mg/kg 2.Koumine (0.28, 7 mg/kg,

8、s.c.) significantly reduces neuropathic pain after nerve injury. Koumine suppressesthe increased Iba-1 protein level 3.REFERENCES1. Zhang X, et al. Apoptotic Effect of Koumine on Human Breast Cancer Cells and the Mechanism Involved. Cell Biochem Biophys. 2015Jun;72(2):411-6.2. Yang J, et al. Effects

9、 of Koumine on Adjuvant- and Collagen-Induced Arthritis in Rats. J Nat Prod. 2016 Oct 28;79(10):2635-2643.3. Jin GL, et al. Koumine Attenuates Neuroglia Activation and Inflammatory Response to Neuropathic Pain. Neural Plast. 2018 Mar25;2018:9347696.McePdfHeightCaution: Product has not been fully validated for medical