在細(xì)胞中，肌肉/內(nèi)質(zhì)鈣 ATP 酶(SERCA)將游離鈣轉(zhuǎn)運(yùn)到肌質(zhì)和內(nèi)質(zhì)網(wǎng)中，降低細(xì)胞內(nèi)鈣水平以阻止通過這種陽離子的信號傳導(dǎo)。毒胡蘿卜素是 SERCAs 鈣轉(zhuǎn)運(yùn)的非競爭性細(xì)胞滲透性抑制劑(IC50值是細(xì)胞類型依賴性的，范圍在2-80nM)。1,2毒胡蘿卜素的抑制導(dǎo)致細(xì)胞內(nèi)鈣的增加，這與細(xì)胞活化，肥大細(xì)胞釋放組胺和增加某些類型的癌細(xì)胞的增殖有關(guān)。1,3,4在體內(nèi)，毒胡蘿卜素和相關(guān)的倍半萜內(nèi)酯具有抗炎和抗癌作用。5,6（參考文末文獻(xiàn)）

艾美捷Thapsigargin技術(shù)信息：

正式名稱：

(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編號：67526-95-8

分子式：C34H50O12

公式重量：650.8

純度：≥97%

配方：結(jié)晶狀固體

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

運(yùn)輸和存儲信息：

儲存：-20°C

運(yùn)輸：美國大陸的室溫；其他地方可能有所不同

穩(wěn)定性：≥ 4年

艾美捷Thapsigargin相關(guān)文獻(xiàn)參考：

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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