毒胡萝卜素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetThapsigarginCat. No.: HY-13433CAS No.: 67526-95-8分式: CHO分量: 650.75作靶点: Calcium Channel; Apoptosis作通路: Membrane Transporter/Ion Channel; Neuronal Signaling; Apoptosis储存式: -20C, sealed storage, away from moisture and light* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 DMSO : 250 mg/mL (384.17 mM

2、; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 1.5367 mL 7.6834 mL 15.3669 mL5 mM 0.3073 mL 1.5367 mL 3.0734 mL10 mM 0.1537 mL 0.7683 mL 1.5367 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现现配，即刻使.体内实验 请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储

3、备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天 使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可 以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.20 mM); Clear solution此案可获得 2.08 mg/mL (3.20 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，

4、混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.20 mM); Clear solution此案可获得 2.08 mg/mL (3.20 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性

5、Thapsigargin种微粒体 Ca2+-ATPase 抑制剂。Thapsigargin 种表征良好的内质应激诱导剂。IC & Target Ca2+-ATPase1体外研究 Thapsigargin (0.001- 1 M; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovialcells in a time- and dose-dependent manner2.Thapsigargin (0.001- 1 M; for 2 and 4 days) induces

6、cell apoptosis in MH7A cells in a time- and dose-dependentmanner2.Thapsigargin (0.001- 1 M; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells2.Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes1.Thapsigargin inhibits the carbachol-evoked Ca2+i-

7、transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC50=4814 nM), is observed in theabsence of a KCl-prestimulation. In contrast, the KCl-evoked Ca2+i-transients displayed only one component with avery lo

8、w sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation3.Cell Proliferation Assay2Cell Line: MH7A human rheumatoid arthritis synovial cellsConcentration: 0.001, 0.1, and 1 MIncubation Time: For 2 and 4 daysResult: Arrested cell prolifera

9、tions in a time- and dose-dependent manner.Apoptosis Analysis2Cell Line: MH7A human rheumatoid arthritis synovial cellsConcentration: 0.001, 0.1, and 1 MIncubation Time: For 2 and 4 daysResult: Induces cell apoptosis in a time- and dose-dependent manner.Western Blot Analysis2Cell Line: MH7A human rh

10、eumatoid arthritis synovial cellsConcentration: 0.001, 0.1, and 1 MIncubation Time: For 2 and 4 daysResult: Impairs mTOR activity and leads to cyclin D1 expressions体内研究Thapsigargin (Injection; 0.25ug/g, 0.5ug/g and 1ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine andpro-inflammator

11、y expression. Thapsigargin is more sensitive to inducing a systemic immune response4.Animal Model: Male Balb/c mice (20-25g) 4Dosage: 0.25ug/g, 0.5ug/g and 1ug/gPage 2 of 3 www.MedChemEAdministration: Injection; 24 hoursResult: Increased of 2 to 5-fold in chemokine and pro-inflammatory expression.户使

12、本产品发表的科研献 ACS Appl Mater Interfaces. 2019 Oct 16;11(41):38190-38204. Vet Microbiol. 2019 Dec;239:108485.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Geiszt M, et al. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Biochem J. 1995 Jan 15;305 (

13、Pt 2):525-8.2. Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014 Feb9;2014:605416.3. Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004Jun 18;1011(2):177-86.4. Abdullahi A, et al. Modeling Acute ER Stress in Vivo and in Vitro. Shock. 2017 Apr;47(4):506-513.McePdfHeightCaution