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毒胡蘿卜素

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  • 公司名稱(chēng)杭州昊鑫生物科技股份有限公司
  • 品       牌MCE
  • 型       號(hào)HY-13433
  • 所  在  地杭州市
  • 廠商性質(zhì)代理商
  • 更新時(shí)間2024/6/26 11:38:31
  • 訪問(wèn)次數(shù)108
產(chǎn)品標(biāo)簽:

Thapsigargin

規(guī)格
1mg1000.00元10000 支可售
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胎牛血清、MCE抑制劑激動(dòng)劑、RNA提取試劑盒、ELISA試劑盒、重組蛋白
CAS號(hào) 67526-95-8 產(chǎn)地 國(guó)產(chǎn)
規(guī)格 1mg 級(jí)別 化工級(jí)
證書(shū) ISO系列證書(shū)
Thapsigargin,內(nèi)質(zhì)網(wǎng)應(yīng)激誘導(dǎo)劑, 是一種微粒體 Ca2+-ATPase 抑制劑。Thapsigargin 能有效抑制不同細(xì)胞類(lèi)型的冠狀病毒 (HCoV-229E、MERS-CoV、SARS-CoV-2) 復(fù)制。
毒胡蘿卜素 產(chǎn)品信息

Thapsigargin (Synonyms: 毒胡蘿卜素)

Thapsigargin,內(nèi)質(zhì)網(wǎng)應(yīng)激誘導(dǎo)劑, 是一種微粒體 Ca2+-ATPase 抑制劑。Thapsigargin 能有效抑制不同細(xì)胞類(lèi)型的冠狀病毒 (HCoV-229E、MERS-CoV、SARS-CoV-2) 復(fù)制。

生物活性

Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types[1][2][3][4][5].


IC50 & Target

Ca2+-ATPase[1]


體外研究(In Vitro)

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[2].
Thapsigargin (0.001-?1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner[2].
Thapsigargin (0.001-?1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells[2].
Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes[1].
Thapsigargin inhibits the carbachol-evoked [Ca2+]i-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 the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca2+]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation[3].
Thapsigargin also phosphorylate p38 MAPK by Ca2+ influx through SOCE, leading to suppression of TNF-α-induced NF-κB phosphorylation.[6].

Cell Proliferation Assay[2]

Cell Line:MH7A human rheumatoid arthritis synovial cells
Concentration:0.001, 0.1, and 1?μM
Incubation Time:For 2 and 4 days
Result:Arrested cell proliferations in a time- and dose-dependent manner.


體內(nèi)研究(In Vivo)

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[4]

Animal Model:Male Balb/c mice (20-25 g)[4]
Dosage:0.25 ug/g, 0.5 ug/g and 1 ug/g
Administration:Injection; 24 hours
Result:Increased of 2 to 5-fold in chemokine and pro-inflammatory expression.


分子量:650.75


Formula:C34H50O12


CAS 號(hào):67526-95-8


中文名稱(chēng):毒胡蘿卜素;毒胡蘿卜內(nèi)酯


運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.


儲(chǔ)存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


溶解性數(shù)據(jù)


In Vitro: 

DMSO : 100 mg/mL (153.67 mM; Need ultrasonic)

配制儲(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM1.5367 mL7.6834 mL15.3669 mL
5 mM0.3073 mL1.5367 mL3.0734 mL
10 mM0.1537 mL0.7683 mL1.5367 mL
*

請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:

——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)依序添加每種溶劑: 10% DMSO    90% saline

    Solubility: 5 mg/mL (7.68 mM); Suspended solution; Need ultrasonic


  • 2.


    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution


  • 3.


    請(qǐng)依序添加每種溶劑: 10% DMSO    90% corn


參考文獻(xiàn)

[1]. Geiszt M, et al. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Biochem J. 1995 Jan 15;305 ( Pt 2):525-8.

[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]. 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.

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

[5]. Mohammed Samer Shaban, et al. Inhibiting coronavirus replication in cultured cells by chemical ER stress. bioRxiv 2020.08.26.266304;

[6]. Junsuke Uwada, et al. Store-operated calcium entry (SOCE) contributes to phosphorylation of p38 MAPK and suppression of TNF-α signalling in the intestinal epithelial cells. Cell Signal. 2019 Nov;63:109358.

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