CAS號	67526-95-8	產(chǎn)地	國產(chǎn)
規(guī)格	1mg	級別	化工級
證書	ISO系列證書

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：67526-95-8

中文名稱：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)

配制儲備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.5367 mL	7.6834 mL	15.3669 mL
5 mM	0.3073 mL	1.5367 mL	3.0734 mL
10 mM	0.1537 mL	0.7683 mL	1.5367 mL

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲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 儲存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： 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.

注：產(chǎn)品僅用于科研