Thapsigargin (Synonyms:毒胡萝卜素)
目录号 : KM9375 CAS No. : 67526-95-8 纯度 : 98%

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冠状病毒 (HCoV-229E、MERS-CoV、SARS-CoV-2) 复制。

规格 价格 是否有货 数量
1mg
In-stock
5mg
In-stock
10mg
In-stock
25mg
In-stock

Other Forms of Rapamycin:

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生物活性

Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.

体外研究

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.
Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner.
Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells.
Thapsigargin inhibits Ca entry into human neutrophil granulocytes.
Thapsigargin inhibits the carbachol-evoked [Ca]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 [Ca]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.

Cell Proliferation Assay

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

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

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
体内研究

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.

Animal Model: Male Balb/c mice (20-25 g)
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.
分子式
C34H50O12
分子量
650.75
CAS号
67526-95-8
中文名称
毒胡萝卜素;毒胡萝卜内酯
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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°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。

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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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