| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: = 99.53%
Thapsigargin is a novel and potent non-competitive inhibitor of the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) and an Endoplasmic Reticulum (ER) stress inducing agent. It is a potent, cell-permeable, IP3-independent intracellular calcium releaser, that works by blocking the transient increase in intracellular Ca2+ induced by angiostatin and endostatin, and inducing apoptosis by disrupting intracellular free Ca2+ levels.
| ln Vitro |
Thapsigargin (0.001-1 μM; for 2 and 4 days) decreases cell proliferation of MH7A human rheumatoid arthritis synoviocytes in a time- and dose-dependent manner [2]. Thapsigargin (0.001-1 μM; for 2 and 4 days). Thapsigargin (0.001-1 μM; for 2 and 4 days) inhibits mTOR activity and increases cyclin D1 expression in MH7A cells [2]. Thapsigargin reduces Ca2+ entrance into human neutrophils [1]. Thapsigargin inhibits carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) KCl prestimulation, but not in the absence. An extra minor component was found with KCl prestimulation, resulting in low fractionation (IC50=4814 nM). In contrast, KCl-induced transient changes in [Ca2+]i exhibited just one component, with a very low shift to Thapsigargin in the absence of the mean of both components (IC50=3343 nM) and the presence of carbachol prestimulation (IC50 =6858 nM)[3]. Additionally, thapsigargin inhibits TNF-α via phosphorylating p38 MAPK through SOCE influx of Ca2+.
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| ln Vivo |
Thapsigargin (injection; 0.25 μg/g, 0.5 μg/g, and 1 μg/g; 24 hours) caused a 2- to 5-fold increase in the expression of proinflammatory chemokines. The ability to elicit systemic immunological responses is more sensitive in thapsigargin [4].
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| Cell Assay |
Cell proliferation assay [2]
Cell Types: MH7A human rheumatoid arthritis synoviocytes Tested Concentrations: 0.001, 0.1 and 1 μM Incubation Duration: 2 and 4 days Experimental Results: Prevents cell proliferation in a. time- and dose-dependent manner. Apoptosis analysis[2] Cell Types: MH7A human rheumatoid arthritis synovial cells Tested Concentrations: 0.001, 0.1 and 1 μM Incubation Duration: 2 days and 4 days Experimental Results: Apoptosis was induced in a time and dose dependent manner. Western Blot Analysis[2] Cell Types: MH7A Human Rheumatoid Arthritis Synovial Cells Tested Concentrations: 0.001, 0.1 and 1 μM Incubation Duration: 2 and 4 Days Experimental Results: Impaired mTOR activity and resulted in cyclin D1 expression |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (20-25 g) [4]
Doses: 0.25 ug/g, 0.5 ug/g, and 1 ug/g Route of Administration: Injection; 24 hour Experimental Results: Increased chemokine and pro-inflammatory expression 2 to 5 times. |
| References |
[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; [6]. Junsuke Uwada, et al. Store-operated calcium entry (SOCE) contributes to phosphorylation of p38 MAPK and suppression of TNF-α signalling in the intestinal epithelial cells. Cell Signal. 2019 Nov;63:109358. |
| Molecular Formula |
C34H50O12
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|---|---|
| Molecular Weight |
650.75
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| CAS # |
67526-95-8
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| SMILES |
C(C(=O)O[C@H]1[C@]2([H])[C@@](OC(C)=O)(C[C@@H]([C@@]3([C@](C)(O)C(=O)O[C@]3(C2=C(C)[C@@H]1OC(=O)/C(/C)=C\C)[H])O)OC(CCC)=O)C)CCCCCC
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~76.83 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (7.68 mM) in 10% DMSO + 90% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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