产品说明书

Thapsigargin

Print
Chemical Structure| 67526-95-8 同义名 : -
CAS号 : 67526-95-8
货号 : A370143
分子式 : C34H50O12
纯度 : 99%+
分子量 : 650.754
MDL号 : MFCD00083511
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(76.83 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 ATP and the divalent cations Mg2+ and Ca2+ regulate K+ stimulation of the Ca2+-transport ATPase of cardiac sarcoplasmic reticulum vesicles[1]. Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types[2]. Thapsigargin (0.001- 1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner. Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner. Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells[3]. Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation[4]. Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01056029 Advanced Solid Tumors Phase 1 Completed - United States, Maryland ... 展开 >> Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins Baltimore, Maryland, United States, 21231 United States, Texas University of Texas, Health Science Center,Cancer Therapy and Research Center San Antonio, Texas, United States, 78229 United States, Wisconsin University of Wisconsin Paul P Carbone Comprehensive Cancer Center Madison, Wisconsin, United States, 53792 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.54mL

0.31mL

0.15mL

7.68mL

1.54mL

0.77mL

15.37mL

3.07mL

1.54mL
参考文献

[1]L R Jones. Mg2+ and ATP effects on K+ activation of the Ca2+-transport ATPase of cardiac sarcoplasmic reticulum. Biochim Biophys Acta. 1979 Oct 19;557(1):230-42.

[2]Geiszt M, et al. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Biochem J. 1995. 305 (Pt 2), 525-8.

[3]Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014. 2014:605416.

[4]Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004. 1011(2), 177-86.

[5]Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017. 47(4), 506-513.