Thapsigargin [67526-95-8]

Cat# TQ0302-1mg

Size : 1mg

Marca : TargetMol


Thapsigargin

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Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.
Thapsigargin
Cas No. 67526-95-8
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.70%
Appearance:Solid
Color:White
COA HNMR HPLC

Product Introduction

Bioactivity
Description
Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.
Targets & IC50
EL4 cells:0.1 μM, CCRF-CEM cells:0.27 μM, HL-60 cells:0.007 μM, PC3 cells:2.4 μM, CCRF S-180 cells:30 nM, K562 cells:0.17 μM, MCF-7 cells:2.3 μM
In vitro
METHODS: Human rheumatoid arthritis synoviocytes MH7A were treated with Thapsigargin (0.001-1 μM) for 2-4 days, and cell proliferation was detected using the SRB.
RESULTS: Thapsigargin inhibited the proliferation of MH7A cells in a time- and dose-dependent manner. [1]
METHODS: Human hepatocellular carcinoma cells HepG2 were treated with Thapsigargin (25-100 nM) for 24 h. Endoplasmic reticulum stress/UPR gene expression was detected by RT-qPCR.
RESULTS: Thapsigargin treatment consistently induced ER stress gene expression only at elevated concentrations of 50 and 100 nM. [2]
In vivo
METHODS: To assay in vivo ER stress-inducing activity, Thapsigargin (0.25-1 μg/g in 150 mM dextrose containing 1% DMSO) was administered as a single intraperitoneal injection to Balb/c mice in order.
RESULTS: Thapsigargin treatment resulted in significant expression of the ER stress markers ATF6 and eIF2α in adipose tissue. thapsigargin treatment failed to induce the expression of most of the ER stress and UPR proteins in the liver. [2]
METHODS: To investigate the antiviral function in vivo, Thapsigargin (30 ng/mouse) was administered by gavage to PR8 virus-infected BALB/c mice once daily for seven days.
RESULTS: Oral administration of Thapsigargin to mice significantly reduced severity and viral shedding and improved survival during infection with the deadly influenza virus. [3]
Cell Research
Cell Line: MH7A human rheumatoid arthritis synovial cells. Concentration: 0.001, 0.1, and 1?μM. Incubation Time: For 2 and 4 days [2]
Animal Research
Animal Model: Male Balb/c mice (20-25g). Dosage: 0.25ug/g, 0.5ug/g and 1ug/g. Administration: Injection; 24 hours [4]
Chemical Properties
Molecular Weight650.75
FormulaC34H50O12
Cas No.67526-95-8
SmilesO(C(CCCCCCC)=O)[C@H]1[C@]2(C([C@]3([C@](O)([C@@H](OC(CCC)=O)C[C@@]2(OC(C)=O)C)[C@](C)(O)C(=O)O3)12)=C(C)[C@@H]1OC(/C(=C\C)/C)=O)12
Relative Density.1.1521 g/cm3 (Estimated)
Storage & Solubility Information
StorageStore at low temperature,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 252.5 mg/mL (388.01 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (7.68 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5367 mL7.6834 mL15.3669 mL76.8344 mL
5 mM0.3073 mL1.5367 mL3.0734 mL15.3669 mL
10 mM0.1537 mL0.7683 mL1.5367 mL7.6834 mL
20 mM0.0768 mL0.3842 mL0.7683 mL3.8417 mL
50 mM0.0307 mL0.1537 mL0.3073 mL1.5367 mL
100 mM0.0154 mL0.0768 mL0.1537 mL0.7683 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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