| Thapsigargin Catalog No.GC11482 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
-
Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| 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. |
|
| Cas No. | 67526-95-8 | SDF | |
| Synonyms | N/A | ||
| Chemical Name | (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 | ||
| Formula | C34H50O12 | M.Wt | 650.76 |
| Solubility | 30mg/ml in ethanol, DMSO, DMF | Storage | Store at -20°C, sealed storage, away from moisture and light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
||
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-
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).