Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca²⁺-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types^{[1][2][3][4][5]}.

Ca²⁺-ATPase^[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

650.75

C₃₄H₅₀O₁₂

67526-95-8

毒胡萝卜素；毒胡萝卜内酯

Room temperature in continental US; may vary elsewhere.

-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)

DMSO : 100 mg/mL (153.67 mM; Need ultrasonic)

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 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。

• [1]. Geiszt M, et al. Thapsigargin inhibits Ca²⁺ entry into human neutrophil granulocytes. Biochem J. 1995 Jan 15;305 ( Pt 2):525-8.

  [2]. Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014 Feb 9;2014:605416.

  [3]. Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004 Jun 18;1011(2):177-86.

  [4]. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.

  [5]. Mohammed Samer Shaban, et al. Inhibiting coronavirus replication in cultured cells by chemical ER stress. bioRxiv 2020.08.26.266304;