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Thapsigargin 目录号 GC11482

sarco-endoplasmic reticulum Ca2+-ATPases inhibitor

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1mg
¥714.00
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5mg
¥2,835.00
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10mg
¥5,177.00
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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment [1,2]:

Cell lines

NG115-401L neural cell line, isolated rat hepatocytes

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

ED50: ~20 nM (NG115-401L neural cell line); ED50 ~80 nM (isolated rat hepatocytes)

Applications

Thapsigargin stimulated a rapid (within 15 s) transient increase in intracellular [Ca2+] in the NG115-401L neural cell line with the ED50 of around 20 nM. In isolated rat hepatocytes, Thapsigargin increased [Ca2+] in a rapid and dose-dependent manner, with an ED50 value of ~80 nM.

Animal experiment [3]:

Animal models

Male C57BL/6 mice with transient middle cerebral artery occlusion (tMCAO)

Dosage form

IC50: 2 to 20 ng, icv injection

Application

Thapsigargin dose-dependently reduced the brain infarct. Thapsigargin (TG) protected mice against ischemia-reperfusion-induced brain injury.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Jackson T R, Patterson S I, Thastrup O, et al. A novel tumour promoter, thapsigargin, transiently increases cytoplasmic free Ca2+ without generation of inositol phosphates in NG115-401L neuronal cells[J]. Biochemical Journal, 1988, 253(1): 81-86.

[2]. Thastrup O, Cullen P J, Drbak B K, et al. Thapsigargin, a tumor promoter, discharges intracellular Ca2+ stores by specific inhibition of the endoplasmic reticulum Ca2 (+)-ATPase[J]. Proceedings of the National Academy of Sciences, 1990, 87(7): 2466-2470.

[3]. Zhang X, Yuan Y, Jiang L, et al. Endoplasmic reticulum stress induced by tunicamycin and thapsigargin protects against transient ischemic brain injury: Involvement of PARK2-dependent mitophagy[J]. Autophagy, 2014, 10(10): 1801-1813.

Chemical Properties

Cas No. 67526-95-8 SDF
别名 N/A
化学名 (3S,3aR,4S,6S,6aR,7S,8S,9bS)-6-acetoxy-4-(butyryloxy)-3,3a-dihydroxy-3,6,9-trimethyl-8-(((Z)-2-methylbut-2-enoyl)oxy)-2-oxo-2,3,3a,4,5,6,6a,7,8,9b-decahydroazuleno[4,5-b]furan-7-yl octanoate
Canonical SMILES O[C@@]([C@H]1OC(CCC)=O)([C@]2(C)O)[C@H](C([C@H]([C@@H]3OC(CCCCCCC)=O)[C@@](C1)(C)OC(C)=O)=C(C)[C@@H]3OC(/C(C)=C\C)=O)OC2=O
分子式 C34H50O12 分子量 650.76
溶解度 30mg/ml in ethanol, DMSO, DMF 储存条件 Desiccate at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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产品描述

In cells, sarco/endoplasmic calcium ATPases (SERCAs) transport free calcium into the sarcoplasmic and endoplasmic reticula, lowering intracellular calcium levels to stop signaling through this cation. Thapsigargin is a non-competitive, cell permeable inhibitor of calcium transport by SERCAs (IC50 values are cell type-dependent and range from ~2-80 nM).1,2 Inhibition of SERCAs leads to an increase in intracellular calcium, which has been linked to cell activation, release of histamine from mast cells, and increased proliferation of certain types of cancer cells.1,3,4 In vivo, thapsigargin and related sesquiterpene lactones have anti-inflammatory and anti-cancer effects.5,6

References:
1. Sabala, P., Czarny, M., Woronczak, J.P., et al. Thapsigargin: Potent inhibitor of Ca2+ transport ATP-ases of endoplasmic and sarcoplasmic reticulum Acta.Biochim.Pol. 40(3), 309-319 (1993).
2. Treiman, M., Caspersen, C., and Christensen, S.B. A tool coming of age: Thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases Trends Pharamacol.Sci. 19(4), 131-135 (1998).
3. Ali, H., Christensen, S.B., Foreman, J.C., et al. The ability of thapsigargin and thapsigargicin to activate cells involved in the inflammatory response British Journal of Pharmacology 85(3), 705-712 (1985).
4. Jackson, T.R., Patterson, S.I., Thastrup, O., et al. A novel tumour promoter, thapsigargin, transiently increases cytoplasmic free Ca2+ without generation of inositol phosphates in NG115-401L neuronal cells Biochemistry Journal 253(1), 81-86 (1988).
5. Christensen, S.B., Skytte, D.M., Deanmeade, S.R., et al. A Trojan horse in drug development: Targeting of thapsigargins towards prostate cancer cells Anticancer Agents Med.Chem. 9(3), 276-294 (2009).
6. Ghantous, A., Gali-Muhtasib, H., Saliba, N.A., et al. What made sesquiterpene lactones reach cancer clinical trials? Drug Discovery Today 15(15-16), 668-678 (2010).