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Thapsigargin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Thapsigargin图片
CAS NO:67526-95-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品名称
毒胡萝卜素
产品介绍
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].

IC50& Target

Ca2+-ATPase[1]

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
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.
分子量

650.75

性状

Solid

Formula

C34H50O12

CAS 号

67526-95-8

中文名称

毒胡萝卜素;毒胡萝卜内酯

结构分类
  • Terpenoids
  • Diterpenoids
来源
  • Plants
  • Umbelliferae
  • Thapsia garganicaL.
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5367 mL7.6834 mL15.3669 mL
5 mM0.3073 mL1.5367 mL3.0734 mL
10 mM0.1537 mL0.7683 mL1.5367 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。

    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。

*以上所有助溶剂都可在本网站选购。