艾美捷Thapsigargin技术信息&文献参考

在细胞中，肌肉/内质钙 ATP 酶(SERCA)将游离钙转运到肌质和内质网中，降低细胞内钙水平以阻止通过这种阳离子的信号传导。毒胡萝卜素是 SERCAs 钙转运的非竞争性细胞渗透性抑制剂(IC50值是细胞类型依赖性的，范围在2-80nM)。1,2毒胡萝卜素的抑制导致细胞内钙的增加，这与细胞活化，肥大细胞释放组胺和增加某些类型的癌细胞的增殖有关。1,3,4在体内，毒胡萝卜素和相关的倍半萜内酯具有抗炎和抗癌作用。5,6（参考文末文献）

艾美捷Thapsigargin技术信息：

正式名称：

(3S,3aS,4R,6R,7S,8R)-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-decahydro-1H-cyclopenta[e]azulen-7-yl octanoate

CAS编号：67526-95-8

分子式：C34H50O12

公式重量：650.8

纯度：≥97%

配方：结晶状固体

溶解度：

DMF: 30 mg/ml

DMSO：30毫克/毫升

乙醇：30毫克/毫升

乙醇：PBS（pH7.2）（1：2）。0.3 mg/ml

运输和存储信息：

储存：-20°C

运输：美国大陆的室温；其他地方可能有所不同

稳定性：≥ 4年

艾美捷Thapsigargin相关文献参考：

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 Pharmacol. 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. Br. J. Pharmacol. 85(3), 705-712 (1985).

4. Jackson, T.R., Patterson, S.I., Thastrup, O., et al. A novel tumour promoter, thapsigargin, transiently increases cylasmic free Ca2+ without generation of inositol phosphates in NG115-401L neuronal cells. Biochem. J. 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 Discov. Today 15(15-16), 668-678 (2010).

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