艾美捷Thapsigargin毒胡萝卜素化学性质&体外研究

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Thapsigargin 是一种有效的、非竞争性的 the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) 的抑制剂，对carbachol诱导的[Ca2+]i瞬变在存不存在KCl预刺激条件下的IC50值分别为0.353 nM和0.448 nM。Thapsigargin 可诱导细胞凋亡。Thapsigargin 提取自植物Thapsia garganica。

艾美捷Thapsigargin技术信息：

正式名称：

(3S,3aS,4R,6R,7S,8R)-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-decahydro-1H-cyclopenta[e]azulen-7-yl octanoate

CAS编号：67526-95-8

分子式：C34H50O12

公式重量：650.8

纯度：≥97%

配方：结晶状固体

溶解度：

DMF: 30 mg/ml

DMSO：30毫克/毫升

乙醇：30毫克/毫升

乙醇：PBS（pH7.2）（1：2）。0.3 mg/ml

运输和存储信息：

储存：-20°C

运输：美国大陆的室温；其他地方可能有所不同

稳定性：≥ 4年

艾美捷Thapsigargin体外研究：

Thapsigargin以时间和剂量依赖的方式阻止MH7A人类类风湿性关节炎滑膜细胞的增殖。

Thapsigargin损害mTOR活性并导致MH7A细胞中细胞周期蛋白D1的表达。

Thapsigargin抑制Ca2+进入人类中性粒细胞。

Thapsigargin在有（IC50=0.353 nM）或没有（IC50=0.448 nM）KCl-prestimulation的情况下，都能抑制卡巴乔诱发的[Ca2+]i-transients，但在没有KCl-prestimulation的情况下，观察到另外一个小的成分，其敏感性要低很多（IC50=4814 nM）。相比之下，lv化物诱发的[Ca2+]i-transients只显示了一个成分，在没有（IC50=3343 nM）和有（IC50=6858 nM）卡巴胆刺激的情况下，对Thapsigargin的敏感性都非常低。

Thapsigargin还通过SOCE的Ca2+流入使p38 MAPK磷酸化，导致TNF-α诱导的NF-κB磷酸化受到抑制。

艾美捷Thapsigargin文献参考：

1. Sabala, P., Czarny, M., Woronczak, J.P., et al. Thapsigargin: Potent inhibitor of Ca2+ transport ATP-ases of endoplasmic and sarcoplasmic reticulum. Acta Biochim. Pol. 40(3), 309-319 (1993).

2. Treiman, M., Caspersen, C., and Christensen, S.B. A tool coming of age: Thapsigargin as an inhibitor of sarco-endoplasmic reticulum Ca2+-ATPases. Trends Pharmacol. Sci. 19(4), 131-135 (1998).

3. Ali, H., Christensen, S.B., Foreman, J.C., et al. The ability of thapsigargin and thapsigargicin to activate cells involved in the inflammatory response. Br. J. Pharmacol. 85(3), 705-712 (1985).

4. 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. Biochem. J. 253(1), 81-86 (1988).

5. Christensen, S.B., Skytte, D.M., Deanmeade, S.R., et al. A Trojan horse in drug development: Targeting of thapsigargins towards prostate cancer cells. Anticancer Agents Med. Chem. 9(3), 276-294 (2009).

6. Ghantous, A., Gali-Muhtasib, H., Saliba, N.A., et al. What made sesquiterpene lactones reach cancer clinical trials? Drug Discov. Today 15(15-16), 668-678 (2010).

艾美捷Thapsigargin文献引用：

1.Nagakannan, P., Islam, M.I., Conrad, M., et al. Cathepsin B is an excutioner of ferroptosis. Biochim. Biophys. Acta Mol. Cell Res. 1868(3), 118928 (2021).

2.Merhi, A., Delrée, P., and Marini, A. The metabolic waste ammonium regulates mTORC2 and mTORC1 signaling. Sci. Rep. 7, 44602 (2017).

3.Wang, A., Huen, S.C., Luan, H.H., et al. Opposing effects of fasting metabolism on tissue tolerance in bacterial and viral inflammation. Cell 166(6), 1512-1525 (2016).

来源：https://www.amyjet.com/products/10522-10.shtml

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TRC丨艾美捷TRC 6-Amino-4-(4-fluorophenyl)-说明书

艾美捷TRC 6-氨基-4-（4-氟苯基）-3-甲基-1,4-二氢吡喃[2,3-c]吡唑-5-碳腈（CAS#89607-37-4）是一种有用的研究化合物。

艾美捷TRC 6-Amino-4-(4-fluorophenyl)-化学性质：

Catalogue NumberA012662

Chemical Name6-Amino-4-(4-fluorophenyl)-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile

CAS Number89607-37-4

Molecular FormulaC14H11FN4O

Molecular Weight270.27

CategoryBuilding Blocks; Miscellaneous;

Applications6-Amino-4-(4-fluorophenyl)-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile (CAS# 89607-37-4) is a useful research chemical compound.

目录编号A012662

化学名称6-氨基-4-（4-氟苯基）-3-甲基-1,4-二氢吡喃[2,3-c]吡唑-5-腈

CAS数字89607-37-4

分子式C14H11FN4O

分子量270.27

类别构建块；混杂的

艾美捷TRC 6-Amino-4-(4-fluorophenyl)-相关研究：

Dimethyl 3-Methylglutaconate

3,7-Dimethyl-1H-indazole-5-carboxylic Acid

1,1-Dimethylethyl Nitrite (~90%)

2-((2,5-Dichlorophenyl)amino)nicotinonitrile

O,O-Dimethyl Methylphosphonate

2-Amino-1-(1-aza-2-(2-(4-chlorophenylthio)-5-nitrophenyl)vinyl)ethene-1,2-dicarbonitrile

2-[(3AR)-1-acetyl-3a-methyl-5-oxooctahydropyrrolo[2,3-b]pyrrol-2-yl]phenyl 5-methyl-3-isoxazolecarboxylate

7-Amino-5-oxo-6-phenethyl-5,6-dihydro[1,6]naphthyridine-8-carbonitrile

5-Amino-3-(4-fluoro-3-methylanilino)-1-methyl-1H-pyrazole-4-carbonitrile

3-Amino-5-(4-fluoro-3-methylanilino)-1-methyl-1H-pyrazole-4-carbonitrile

TRC拥有多领域的化学专业技术，包括碳水化合物，芳香烃，硝化物，硫化物以及放射同位素和稳定同位素标记化合物，各类标准品等。艾美捷科技是TRC的中国代理商，为科研工作者提供优质的产品与服务。

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 3-氨基-N-（2,5-二甲氧基苯基）说明书

艾美捷TRC 3-氨基-N-（2,5-二甲氧基苯基）苯甲酰胺（CAS#81882-65-7）是一种有用的研究化合物。

艾美捷TRC 3-氨基-N-（2,5-二甲氧基苯基）苯甲酰胺化学性质：

Catalogue NumberA013130

Chemical Name3-Amino-N-(2,5-dimethoxyphenyl)benzamide

CAS Number81882-65-7

Molecular FormulaC15H16N2O3

Molecular Weight272.31

Applications3-Amino-N-(2,5-dimethoxyphenyl)benzamide (CAS# 81882-65-7) is a useful research chemical compound.

目录编号A013130

化学名称3-氨基-N-（2,5-二甲氧基苯基）苯甲酰胺

CAS编号81882-65-7

分子式C15H16N2O3

分子量272.31

艾美捷TRC 3-氨基-N-（2,5-二甲氧基苯基）苯甲酰胺相关研究：

2-Acetonyl-5-methyl-1,3,4-oxadiazole

3-Amino-N-[2-(1-cyclohexen-1-yl)ethyl]benzamide

3-Amino-N-(5-chloro-2-methylphenyl)benzamide

4-Amino-N-(4-chlorophenyl)benzamide

2-Amino-1-(1-aza-2-(2-(4-chlorophenylthio)-5-nitrophenyl)vinyl)ethene-1,2-dicarbonitrile

2-[(3AR)-1-acetyl-3a-methyl-5-oxooctahydropyrrolo[2,3-b]pyrrol-2-yl]phenyl 5-methyl-3-isoxazolecarboxylate

7-Amino-5-oxo-6-phenethyl-5,6-dihydro[1,6]naphthyridine-8-carbonitrile

5-Amino-3-(4-fluoro-3-methylanilino)-1-methyl-1H-pyrazole-4-carbonitrile

3-Amino-5-(4-fluoro-3-methylanilino)-1-methyl-1H-pyrazole-4-carbonitrile

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 4-（6-氨基吡啶-3-基）苯甲酸说明书

艾美捷TRC 4-（6-氨基吡啶-3-基）苯甲酸（CAS 222986-51-8）是一种有用的研究化合物。

艾美捷TRC 4-（6-氨基吡啶-3-基）苯甲酸化学性质：

Catalogue NumberA013316

Chemical Name4-(6-Aminopyridin-3-yl)benzoic acid

CAS Number222986-51-8

Molecular FormulaC12H10N2O2

Molecular Weight214.23

CategoryBuilding Blocks; Miscellaneous;

Applications4-(6-Aminopyridin-3-yl)benzoic acid (CAS# 222986-51-8) is a useful research chemical compound.

目录编号A013316

化学名称4-（6-氨基吡啶-3-基）苯甲酸

CAS数字222986-51-8

分子式C12H10N2O2

分子量214.23

类别构建块；混杂的

艾美捷TRC 4-（6-氨基吡啶-3-基）苯甲酸相关研究：

2-Acetonyl-5-methyl-1,3,4-oxadiazole

3-Amino-N-[2-(1-cyclohexen-1-yl)ethyl]benzamide

3-Amino-N-(5-chloro-2-methylphenyl)benzamide

4-Amino-N-(4-chlorophenyl)benzamide

2-[(3AR)-1-acetyl-3a-methyl-5-oxooctahydropyrrolo[2,3-b]pyrrol-2-yl]phenyl 5-methyl-3-isoxazolecarboxylate

7-Amino-5-oxo-6-phenethyl-5,6-dihydro[1,6]naphthyridine-8-carbonitrile

5-Amino-3-(4-fluoro-3-methylanilino)-1-methyl-1H-pyrazole-4-carbonitrile

3-Amino-5-(4-fluoro-3-methylanilino)-1-methyl-1H-pyrazole-4-carbonitrile

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 2-氮杂环丁烷-1-基-说明书

艾美捷TRC 2-氮杂环丁烷-1-基-5-（4,4,5,5-四甲基-[1,3,2]二氧苯并呋喃-2-基）-吡啶（CAS 1257553-70-0）是一种有用的研究化合物。

艾美捷TRC 2-氮杂环丁烷-1-基-化学性质：

Catalogue NumberA013358

Chemical Name2-Azetidin-1-yl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyridine

CAS Number1257553-70-0

Molecular FormulaC14H21BN2O2

Molecular Weight260.15

CategoryBuilding Blocks; Miscellaneous;

Applications2-Azetidin-1-yl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyridine (CAS# 1257553-70-0) is a useful research chemical compound.

目录编号A013358

化学名称2-氮杂环丁烷-1-基-5-（4,4,5,5-四甲基-[1,3,2]二氧杂硼烷-2-基）-吡啶

CAS数字1257553-70-0

分子式C14H21BN2O2

分子量260.15

类别构建块；混杂的

艾美捷TRC 2-氮杂环丁烷-1-基-相关研究：

Dimethyl 3-Methylglutaconate

3,7-Dimethyl-1H-indazole-5-carboxylic Acid

1,1-Dimethylethyl Nitrite (~90%)

2-((2,5-Dichlorophenyl)amino)nicotinonitrile

O,O-Dimethyl Methylphosphonate

7-Amino-3-methylbenzo[d]isoxazol-6-ol

5-Amino-2-bromo-4-methoxybenzoic acid

4-Amino-3,4-dihydronaphthalen-1(2H)-one

4-(6-Aminopyridin-3-yl)benzoic acid

5-(4-Aminophenoxy)pyridine-2-carboxylic acid dihydrochloride

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 4-Azido-2-说明书

艾美捷TRC 4-Azido-2-（CAS#2279124-17-1）是一种有用的研究化合物。

艾美捷TRC 4-Azido-2-化学性质：

Catalogue NumberA013400

Chemical Name4-Azido-2-trifluoromethylbenzoic acid

CAS Number2279124-17-1

Molecular FormulaC8H4F3N3O2

Molecular Weight231.14

CategoryBuilding Blocks; Miscellaneous;

Applications4-Azido-2-trifluoromethylbenzoic acid (CAS# 2279124-17-1) is a useful research chemical compound.

目录编号A013400

化学名称4-Azido-2-trifluoromethylbenzoic acid

CAS编号2729124-17-1

分子式C8H4F3N3O2

分子量231.14

类别构建块；混杂的

艾美捷TRC 4-Azido-2-相关研究：

Alternariol

交链孢酚/交替醇 A575760

Atorvastatin Calcium Salt

阿托伐他汀(钙盐) A791750

PP-3-MCPD

3-氯-1,2-丙二醇-二棕榈酸酯 B515200

Celecoxib

塞来昔布 C251000

(Dimethylamino)guanosine

N,N-二甲基鸟嘌呤核苷 D460850

O-α-D-Glucosylglycerol

甘油葡糖苷/甘油葡萄糖苷 H943140

Meropenem-d6 (>90%)

美罗培南-D6 M225617

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 5-乙酰基-3-噻吩硼酸基说明书

艾美捷TRC （5-乙酰基-3-噻吩基）硼酸（CAS 942190-74-1）是一种有用的研究化合物。

艾美捷TRC 5-乙酰基-3-噻吩硼酸化学性质：

Catalogue NumberA013535

Chemical Name(5-Acetyl-3-thienyl)boronic acid

CAS Number942190-74-1

Molecular FormulaC6H7BO3S

Molecular Weight170

Applications(5-Acetyl-3-thienyl)boronic acid (CAS# 942190-74-1) is a useful research chemical compound.

目录编号A013535

化学名称（5-乙酰-3-噻吩基）硼酸

CAS编号942190-74-1

分子式C6H7BO3S

分子量170

艾美捷TRC 5-乙酰基-3-噻吩硼酸相关研究：

1-Acetyl-3(5)-heptafluoropropyl-5(3)-methyl-4-nitropyrazole

2-Amino-1-[4-(2-ethoxyphenyl)piperazin-1-yl]ethanone

3-(2-Aminoethyl)-2-methyl-1H-indole-5-carbonitrile hydrochloride

2-Amino-N-(3,5-dimethylphenyl)-acetamide

5-Amino-1-(4-bromophenyl)-1H-pyrazole-4-carboxylic acid ethyl ester

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 3-Azepan-2-yl-说明书

艾美捷TRC 3-Azepan-2-yl-（CAS 1210740-44-5）是一种有用的研究化合物。

艾美捷TRC 3-Azepan-2-yl-化学性质：

Catalogue NumberA013550

Chemical Name3-Azepan-2-yl-quinoline monoacetate

CAS Number1210740-44-5

Molecular FormulaC17H22N2O2

Molecular Weight286.38

CategoryBuilding Blocks; Miscellaneous;

Applications3-Azepan-2-yl-quinoline monoacetate (CAS# 1210740-44-5) is a useful research chemical compound.

目录编号A013550

化学名称3-Azepan-2-yl-

CAS数字1210740-44-5

分子式C17H22N2O2

分子量286.38

类别构建块；混杂的

艾美捷TRC 3-Azepan-2-yl-相关研究：

Dimethyl 3-Methylglutaconate

3,7-Dimethyl-1H-indazole-5-carboxylic Acid

1,1-Dimethylethyl Nitrite (~90%)

2-((2,5-Dichlorophenyl)amino)nicotinonitrile

O,O-Dimethyl Methylphosphonate

1-Acetyl-3(5)-heptafluoropropyl-5(3)-methyl-4-nitropyrazole

2-Amino-1-[4-(2-ethoxyphenyl)piperazin-1-yl]ethanone

3-(2-Aminoethyl)-2-methyl-1H-indole-5-carbonitrile hydrochloride

2-Amino-N-(3,5-dimethylphenyl)-acetamide

5-Amino-1-(4-bromophenyl)-1H-pyrazole-4-carboxylic acid ethyl ester

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC 3-甲基戊二酸二甲酯说明书

艾美捷TRC 3-甲基戊二酸二甲酯可诱导大鼠纹状体和肝脏的氧化损伤。还用于制备具有保幼激素活性的昆虫生长调节剂。

艾美捷TRC 3-甲基戊二酸二甲酯化学性质：

Catalogue NumberD474725

Chemical NameDimethyl 3-Methylglutaconate

Synonyms3-Methyl-2-pentenedioic Acid Dimethyl Ester; 3-Methyl-glutaconic Acid Dimethyl Ester ; Dimethyl 3-Methylglutaconate; Dimethyl β-Methylglutaconate

CAS Number52313-87-8

Molecular FormulaC8H12O4

AppearanceClear Colourless to Pale Yellow Oil

Melting PointN/A

Molecular Weight172.18

StorageRefrigerator

SolubilityChloroform, Methanol

CategoryBuilding Blocks; Miscellaneous; Pharmaceutical/API Drug Impurities/Metabolites;

ApplicationsDimethyl 3-Methylglutaconate are shown to induce oxidative damage on striatum and the liver in rats. Also used in the preparation of insect growth regulators with juvenile hormone activity.

ReferencesLeipnitz, G. et al.: Int. J. Dev. Neuro., 27, 351 (2009); Henrick, C. et al.: J. Org. Chem., 40, 1 (1975);

目录编号D474725

化学名称3-甲基戊二酸二甲酯

同义词3-甲基-2-戊二酸二甲酯；3-甲基-戊二酸二甲酯；3-甲基戊二酸二甲酯；β-甲基戊二酸二甲酯

CAS编号52313-87-8

分子式C8H12O4

外观清澈无色至淡黄色油

熔点不适用

分子量172.18

存储冰箱

溶解度lv仿，甲醇

类别构建块；混杂的药物/原料药药物杂质/代谢物；

参考文献Leipnitz，G.等人：Int.J.Dev.Neuro。，27, 351 (2009); Henrick，C.等人：J.Org.Chem。，40, 1 (1975);

艾美捷TRC 3-甲基戊二酸二甲酯相关研究：

(2'S)-Nicotine 1-Oxide-d4

rac-Nicotine 1-Oxide-d4

N,N-Diethyl-2,2,2-trifluoroacetamide

3-Isobutylaniline

a,a-Dimethyl-4-[(methylamino)methyl]-2-thiazolemethanol Hydrochloride

2,4-Dichloro-6-methyl-7H-pyrrolo[2,3-d]pyrimidine

Dimethyl 2,2'-((2-(2-(2-(Bis(2-methoxy-2-oxoethyl)amino)-5-(chlorocarbonyl)phenoxy)ethoxy)-4-methylphenyl)azanediyl)diacetate

2-(2,4-Dichlorophenyl)thiazole-4-carboxylic Acid

4,5-Dimethylnicotinonitrile

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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TRC丨艾美捷TRC a，a-二甲基-4-说明书

艾美捷TRC a，a-二甲基-4-用途：A Cobistat（C633150）杂质。Cobistat是一种HIV蛋白酶抑制剂，已与低剂量利托那韦（R535000）作为药物增效剂联合使用，显著提高了其血浆浓度。

艾美捷TRC a，a-二甲基-4-化学性质：

Catalogue NumberD474700

Chemical Namea,a-Dimethyl-4-[(methylamino)methyl]-2-thiazolemethanol Hydrochloride

Alternate CAS #Free Base: 1051463-24-1

Molecular FormulaC₈H₁₅ClN₂OS

AppearanceDark Brown Gel to Light Brown Solid

Molecular Weight222.74

Storage-20°C, Inert atmosphere, Light sensitive

SolubilityChloroform, DMSO, Methanol

CategoryStandards; Pharmaceutical/API Drug Impurities/Metabolites;

ApplicationsA Cobicistat (C633150) impurity. Cobicistat is a HIV protease inhibitor and have been coadministered with low-dose ritonavir (R535000) as a pharmacoenhancer, significantly increasing their plasma concentrations.

ReferencesVon, H., Exp. Rev. Clin. Pharmacol., 5, 557 (2012); Lepist, E.I., et al.: Antimicrob. Agent. Chemother., 56, 5409 (2012); Orr, S.T.M., et al.: J. Med. Chem., 55, 4896 (2012);

目录编号D474700

化学名称a，a-二甲基-4-[（甲氨基）甲基]-2-噻唑甲醇盐酸盐

备用CAS自由基：1051463-24-1

分子式C₈H₁₅ClN公司₂操作系统

外观深棕色凝胶至浅棕色固体

分子量222.74

储存-20°C，惰性气氛，光敏

溶解度氯仿、DMSO、甲醇

类别标准；药物/原料药药物杂质/代谢物；

参考文献Von，H.，Exp.Rev.Clin。药理学。，5, 557 (2012); Lepist，E.I.等人：抗微生物。代理人Chemother。，56, 5409 (2012); Orr，S.T.M.等人：《医学化学杂志》。，55, 4896 (2012);

艾美捷TRC a，a-二甲基-4-相关研究：

(2'S)-Nicotine 1-Oxide-d4

rac-Nicotine 1-Oxide-d4

1,1-Dimethyl-4-phenylpiperazinium Iodide

1,3-Dioleoylglycerol-d5

Diphenyl Terephthalate

2,4-Dichloro-6-methyl-7H-pyrrolo[2,3-d]pyrimidine

Dimethyl 2,2'-((2-(2-(2-(Bis(2-methoxy-2-oxoethyl)amino)-5-(chlorocarbonyl)phenoxy)ethoxy)-4-methylphenyl)azanediyl)diacetate

2-(2,4-Dichlorophenyl)thiazole-4-carboxylic Acid

4,5-Dimethylnicotinonitrile

2,5-Dichloro-4-methylpyrimidine

来源：https://www.amyjet.com/brand/Toronto-Research-Chemicals.shtml

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