规格 | 价格 | 库存 | 数量 |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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体外研究 (In Vitro) |
Shikonin,TMEM16A 氯通道抑制剂,IC50 为 6.5 μM[1]。此外,紫草激肽特异性抑制 PKM2 [2]。此外,它还可以阻止核因子-κB (NF-κB) 通路的激活并抑制肿瘤坏死因子-α (TNF-α)。与对照相比,当暴露于浓度大于 50 μM 的紫草素时,正常人角质形成细胞 (NHK) 的活力显着降低 (P<0.05)。紫草素预处理两小时可抑制 TNF-α 诱导的 NF-κB p65 核转位 [3]。用 5 和 7.5 μM 紫草素处理 12 小时后,细胞活力显着降低。与 0 小时组相比,两种细胞系的抑制作用也显示出时间依赖性模式。结果发现,在24至48小时的时间段内,5μM紫草素比2.5μM紫草素具有更强的抑制作用。当U87和U251细胞用2.5、5和7.5 μM紫草素处理24和48小时(p<0.01)时,它们的侵袭性远低于对照组[4]。
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体内研究 (In Vivo) |
与骨关节炎组相比,紫草素显着阻止骨关节炎大鼠模型中IL-1β和TNF-α表达水平的升高(P<0.01)。在骨关节炎大鼠模型中,与骨关节炎组相比,紫草素显着降低了 NF-κB 蛋白表达量(P<0.01)。在用紫草素治疗的大鼠骨关节炎模型中,与骨关节炎组相比,诱导的iNOS水平降低(P<0.01)。与骨关节炎组相比,紫草素治疗显着降低了骨关节炎大鼠模型中COX-2蛋白表达的增加(P<0.01)。紫草素治疗的骨关节炎大鼠模型中caspase-3活性的增加明显低于骨关节炎组(P<0.01)。接受紫草素治疗后,骨关节炎组大鼠骨关节炎模型中Akt磷酸化显着恢复(P<0.01)[5]。
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参考文献 |
[1]. Jiang Y et al. Shikonin Inhibits Intestinal Calcium-Activated Chloride Channels and Prevents Rotaviral Diarrhea. Front Pharmacol. 2016 Aug 23;7:270.
[2]. Li W, et al. Shikonin Suppresses Skin Carcinogenesis via Inhibiting Cell Proliferation. PLoS One. 2015 May 11;10(5):e0126459. [3]. Yan Y, et al. Shikonin Promotes Skin Cell Proliferation and Inhibits Nuclear Factor-κB Translocation via Proteasome Inhibition In Vitro. Chin Med J (Engl). 2015 Aug 20;128(16):2228-33. [4]. Zhang FY, et al. Shikonin Inhibits the Migration and Invasion of Human Glioblastoma Cells by Targeting Phosphorylated β-Catenin and Phosphorylated PI3K/Akt: A Potential Mechanism for the Anti-Glioma Efficacy of a Traditional Chinese Herbal Medicine. Int J Mol Sci. 2015 Oct 9;16(10):23823-48. [5]. Fu D, et al. Shikonin inhibits inflammation and chondrocyte apoptosis by regulation of the PI3K/Akt signaling pathway in a rat model of osteoarthritis. Exp Ther Med. 2016 Oct;12(4):2735-2740. [6]. Kathleen M McAndrews, et al. Mechanisms associated with biogenesis of exosomes in cancer. Mol Cancer. 2019 Mar 30;18(1):52. [7]. Jernej Zorman, et al. Shikonin Suppresses NLRP3 and AIM2 Inflammasomes by Direct Inhibition of Caspase-1. PLoS One. 2016 Jul 28;11(7):e0159826 |
分子式 |
C16H16O5
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分子量 |
288.3
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精确质量 |
288.0998
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CAS号 |
517-89-5
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相关CAS号 |
(-)-Alkannin;517-88-4;Alkannin;23444-65-7;(Rac)-Shikonin;54952-43-1
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SMILES |
O([H])[C@]([H])(C([H])([H])/C(/[H])=C(\C([H])([H])[H])/C([H])([H])[H])C1=C([H])C(C2=C(C([H])=C([H])C(=C2C1=O)O[H])O[H])=O
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别名 |
Tokyo Violet Shikonin
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO : ~125 mg/mL (~433.58 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 30 mg/mL (104.06 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 3.4686 mL | 17.3430 mL | 34.6861 mL | |
5 mM | 0.6937 mL | 3.4686 mL | 6.9372 mL | |
10 mM | 0.3469 mL | 1.7343 mL | 3.4686 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。