Thapsigargin,内质网应激诱导剂, 是一种微粒体Ca2+-ATPase抑制剂。Thapsigargin 能有效抑制不同细胞类型的病毒 (HCoV-229E、MERS-CoV、COVID-19) 复制。
生物活性 | Thapsigargin, anendoplasmic reticulum (ER) stressinducer, is an inhibitor of microsomalCa2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types[1][2][3][4][5]. |
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体外研究 (In Vitro) | Thapsigargin (0.001- 1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner[2]. Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner[2]. Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells[2]. Thapsigargin inhibits Ca2+entry into human neutrophil granulocytes[1]. Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC50=4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca2+]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation[3]. Thapsigargin also phosphorylate p38 MAPK by Ca2+influx through SOCE, leading to suppression of TNF-α-induced NF-κB phosphorylation.[6].
Cell Proliferation Assay[2] Cell Line: | MH7A human rheumatoid arthritis synovial cells | Concentration: | 0.001, 0.1, and 1 μM | Incubation Time: | For 2 and 4 days | Result: | Arrested cell proliferations in a time- and dose-dependent manner. |
Apoptosis Analysis[2] Cell Line: | MH7A human rheumatoid arthritis synovial cells | Concentration: | 0.001, 0.1, and 1 μM | Incubation Time: | For 2 and 4 days | Result: | Induces cell apoptosis in a time- and dose-dependent manner. |
Western Blot Analysis[2] Cell Line: | MH7A human rheumatoid arthritis synovial cells | Concentration: | 0.001, 0.1, and 1 μM | Incubation Time: | For 2 and 4 days | Result: | Impairs mTOR activity and leads to cyclin D1 expressions |
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体内研究 (In Vivo) | Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response[4].
Animal Model: | Male Balb/c mice (20-25 g)[4] | Dosage: | 0.25 ug/g, 0.5 ug/g and 1 ug/g | Administration: | Injection; 24 hours | Result: | Increased of 2 to 5-fold in chemokine and pro-inflammatory expression. |
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来源 | - Plants
- Umbelliferae
- Thapsia garganicaL.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(153.67 mM;Need ultrasonic) H2O : 25 mg/mL(38.42 mM;Need ultrasonic) 配制储备液 1 mM | 1.5367 mL | 7.6834 mL | 15.3669 mL | 5 mM | 0.3073 mL | 1.5367 mL | 3.0734 mL | 10 mM | 0.1537 mL | 0.7683 mL | 1.5367 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;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 90% saline Solubility: 5 mg/mL (7.68 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 (3.20 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.20 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%corn oil Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (3.20 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。 *以上所有助溶剂都可在本网站选购。
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