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紫草素  ≥98%(HPLC),分析标准品

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包装规格：20mg in glass bottle
产品简介：一种中草药紫草的主要成分。是有效的 TMEM16A 氯化物通道 (chloride channel) 抑制剂，IC50 为 6.5 μM。Shikonin 是一种特异的丙酮酸激酶 M2 (PKM2) 抑制剂，还可以抑制 TNF-α 和 NF-κB途径。Shikonin 通过抑制糖酵解降低外泌体 (exosome) 的分泌。Shikonin 抑制 AIM2炎性体活化。
溶解性：DMSO :125 mg/mL (433.58 mM; Need ultrasonic)
储备液保存：-80°C, 6 months -20°C, 1 month
体内实验：1、请依序添加每种溶剂： 0.5% CMC-Na/saline water Solubility: 30 mg/mL (104.06 mM); Suspended solution; Need ultrasonic 2、请依序添加每种溶剂： 10% DMSO→ 40% PEG300→ 5% Tween-80→ 45% saline Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution 此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 3、请依序添加每种溶剂： 10% DMSO→ 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution 此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 4、请依序添加每种溶剂： 10% DMSO→ 90% corn oil Solubility: ≥ 2.08 mg/mL (7.21 mM); Clear solution 此方案可获得 ≥ 2.08 mg/mL (7.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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。
靶点：TMEM16A chloride channel;PKM2;NF-κB;6.5 μM (IC50)
体外研究：Shikonin is an inhibitor of TMEM16A chloride channel with an IC50 of 6.5 μM. Shikonin is also a specific inhibitor of PKM2 and can also inhibit tumor necrosis factor-α (TNF-α) and prevent activation of nuclear factor-κB (NF-κB) pathway. Shikonin at concentrations higher than 50 μM significantly inhibits ormal human keratinocytes (NHKs) viability, compare with that of control (P<0.05). Pretreatment with Shikonin for 2 h attenuates TNF-α-induced NF-κB p65 nuclear translocation. Treatments of Shikonin at 5 and 7.5 μM significantly inhibit the cell viability starting from 12 h and the inhibitory effects are presented in time-dependent patterns compare with the 0 h group in both cell lines. It is found that 5 μM Shikonin displays greater inhibition compare to 2.5 μM at the time points from 24 to 48 h. The invasiveness of U87 and U251 cells is significantly attenuated when treated with Shikonin at 2.5, 5, and 7.5 μM compare with the control group at 24 and 48 h (p<0.01).
体内研究：Shikonin significantly inhibits the increase in IL-1β and TNF-α expression levels in the rat model of osteoarthritis, compare with those in the osteoarthritis group (P<0.01). The NF-κB protein expression level is significantly suppressed by Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The induction of the iNOS level is suppressed by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The administration of Shikonin markedly weakens the up-regulation of COX-2 protein expression in the rat model of osteoarthritis, as compare with that in the osteoarthritis group (P<0.01). The elevation of caspase-3 activity is significantly reduced by Shikonin treatment in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01). The downregulation of Akt phosphorylation is also significantly recovered by treatment with Shikonin in the rat model of osteoarthritis, compare with that in the osteoarthritis group (P<0.01).
保存条件：2-8℃
注意事项：1、为了您的安全和健康，请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。

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