Thapsigargin

立即咨询

Thapsigargin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

67526-95-8

包装与价格：

包装	价格(元)
1mg	电议
5mg	电议
10mg	电议

产品介绍

化学性质

Physical Appearance	A crystalline solid
Storage	Desiccate at -20°C
M.Wt	650.76
Cas No.	67526-95-8
Formula	C₃₄H₅₀O₁₂
Solubility	Soluble in DMSO
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
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

Thapsigargin is an inhibitor of microsomal Ca²⁺-ATPase, Thapsigargin inhibits the carbachol-evoked [Ca²⁺]i-transients with IC50 value of 0.353 nM [1].

Thapsigargin may induce cell apoptosis in MH7A cells in a time- and dose-dependent manner, and the percentages of cell death reached 44.6% at thapsigargin concentration of 1 μM treated for 4 days compared to the control. The protein and mRNA levels of cyclin D1 decreased gradually with the increasing of thapsigargin concentration and treatment times [2].

In regards to vivo results, tunicamycin is superior in not only inducing ER stress but also recapturing the metabolic alterations associated with ER stress [3].

References:

[1].Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004 Jun 18;1011(2):177-86.

[2].Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014 Feb 9;2014:605416.

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

试验操作

细胞实验 [1,2]:
细胞系	NG115-401L神经细胞系，分离大鼠肝细胞
溶解方法	该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液，可在37°C下孵育10分钟，随后在超声波浴中摇匀。-20°C以下可储存数月。
反应条件	ED50: ～20 nM （NG115-401L神经细胞系）； ED50:～80 nM（大鼠肝细胞）
应用	在NG115-401L神经细胞系中，Thapsigargin刺激细胞内[Ca²⁺]的快速瞬时增加（15秒内），ED50约为20 nM。在分离的大鼠肝细胞中，Thapsigargin以快速和剂量依赖的方式增加[Ca²⁺]，ED50值约为80 nM。
动物实验 [3]:
动物模型	伴有短暂大脑中动脉闭塞（tMCAO）的雄性C57BL/6小鼠
给药剂量	IC50: 2-20 ng，脑室内注射
应用	Thapsigargin以剂量依赖性方式减少脑梗塞。Thapsigargin保护小鼠免受缺血再灌注诱发的脑损伤。
注意事项	由于实验环境的不同，实际溶解度可能与理论值略有不同，请测试室内所有化合物的溶解度。
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.