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依布硒

硒有机化合物，抗氧化剂，谷胱甘肽过氧化物酶的模拟物

规格或纯度: ≥98.0%(GC)

CAS编号: 60940-34-3
分子式: C₁₃H₉NOSe
分子量: 274.18
MDL号: MFCD00210937
PubChem编号: 3194

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货号 (SKU)	包装规格	是否现货	价格	数量
P137293-5mg	5mg	现货
P137293-25mg	25mg	现货
P137293-100mg	100mg	现货
P137293-500mg	500mg	现货

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CoV Papain-like protease Inhibitor

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基本描述

规格或纯度	≥98.0%(GC)
英文名称	Ebselen
别名	2-苯基-1,2-苯并异硒唑-3(2H)-酮
英文别名	2-Phenyl-1,2-benzisoselenazol-3(2H)-one; Harmokisane; Ebselene;2-Phenyl-1，2-benzoselenazol-3-one
生化机理	An organo-selenium compound possessing antioxidant properties. Inhibits mammalian lipoxygenases in the absence of thiol groups, and glutathione S-transferase and papain via the interaction with cysteine residues. Also inhibits indoleamine 2,3-dioxygenase by covalently modifying a cysteine residue, the effect being reversible with dithiothreitol.1 Inhibits oxidation of low density lipoproteins (LDL).Seleno-organic compound, antioxidant, mimic of glutathione peroxidase. Inhibitor of lipoxygenases, NO synthases, NADPH oxidase, protein kinase C and H+/K(+)-ATPase producing anti-inflammatory effects.
应用	An inhibitor of 5-LO, 15-LO, Cox, NADPH, and NADPH oxidase.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。
产品介绍	Ebselen is an interesting organoselenium compound displaying antiinflammatory and antioxidant properties. Ebselen is shown to inhibit the 5-lipoxygenase (5-LO) and 15-lipoxygenase (15-LO) enzymes in the absence of glutathione. Ebselen also inhibits Cox (cyclooxygenase), PKC (protein kinase C), DECR1 (NADPH), and Mox-1 (NADPH oxidase). The oxidation of low density lipoproteins by free radicals is suppressed by the antioxidant action of Ebselen. Ebselen is an inhibitor of Cox-1, Cox-2, NOS, GST and IDO.An inhibitor of 5-LO, 15-LO, Cox, NADPH, and NADPH oxidase. Ebselen is an interesting organoselenium compound displaying antiinflammatory and antioxidant properties. Ebselen is shown to inhibit the 5-lipoxygenase (5-LO) and 15-lipoxygenase (15-LO) enzymes in the absence of glutathione. Ebselen also inhibits Cox (cyclooxygenase), PKC (protein kinase C), DECR1 (NADPH), and Mox-1 (NADPH oxidase). The oxidation of low density lipoproteins by free radicals is suppressed by the antioxidant action of Ebselen. Ebselen is an inhibitor of Cox-1, Cox-2, NOS, GST and IDO. An inhibitor of 5-LO, 15-LO, Cox, NADPH, and NADPH oxidase. application： Ebselen has been used as a:voltage-dependent calcium channels (VDCCs) blocker；glutathione peroxidase mimetic to test its inhibitory effect on contraction-mediated deoxy glucose (2-DG) uptake in mouse；extensor digitorum longus (fast-twitch) muscle glucocerebrosidase inhibitor；hepatitis C virus helicase inhibitor

名称和标识符

IUPAC Name	2-phenyl-1,2-benzoselenazol-3-one
INCHI	InChI=1S/C13H9NOSe/c15-13-11-8-4-5-9-12(11)16-14(13)10-6-2-1-3-7-10/h1-9H
InChi Key	DYEFUKCXAQOFHX-UHFFFAOYSA-N
Canonical SMILES	C1=CC=C(C=C1)N2C(=O)C3=CC=CC=C3[Se]2
分子式	C₁₃H₉NOSe
PubChem CID	3194
分子量	274.18

数据库链接

PubChem CID	3194
CAS Registry No.	60940-34-3
Wikipedia	Ebselen
DrugBank Ligand	DB12610

化学和物理性质

溶解性	Solubility in water: insoluble Solubility in other solvents: soluble in methanol, ethanol, THF, ethyl acetate, DMSO
敏感性	对热敏感
熔点	183 °C

安全信息

象形图	Toxic Health Hazard Environmental Hazard
信号词	Danger
危险声明	H301: Toxic if swallowed H331: Toxic if inhaled H373: Causes damage to organs through prolonged or repeated exposure H400: Very toxic to aquatic life H410: Very toxic to aquatic life with long lasting effects
预防措施声明	P261,P273,P321,P405,P501,P264,P260,P271,P270,P304+P340,P403+P233,P391,P330,P301+P316,P316,P319
WGK Germany	3
Merck Index	3486

靶标

Target ID	3132
名称	CoV Papain-like protease
缩写名	SHP2
家族	Coronavirus (CoV) proteins
别名	MB-IRK3
UniProtKB	P0DTC1 (SARS-CoV-2)

关联配体

Ligand ID	10583
名称	ebselen
类别	Synthetic organic
学名	2-phenyl-1,2-benzoselenazol-3-one
生物活性评价	Ebselen completely blocked Carbachol-induced calcium mobilization (via the G_q-coupled muscarinic M₃ receptor) as well as ADP-induced calcium mobilization (via the P2Y₁ receptor) in recombinant 1321N1 astrocytoma cells with pIC₅₀ values of 5.36 and 5.63, respectively .
评价	A synthetic organoselenium molecule with anti-inflammatory, anti-oxidant and cytoprotective activity, characterised as a small molecule G_q protein inhibitor. A bioRxiv preprint suggests that ebselen is a low micromolar, covalent, fast-binding inhibitor of papain-like protease (PL-pro) from SARS-CoV-2 . This study also reports that ebselen is less active against SARS-CoV, and binds more slowly to this enzyme homologue.

参考文献

1. Kuschak M, Namasivayam V, Rafehi M, Voss JH, Garg J, Schlegel JG, Abdelrahman A, Kehraus S, Reher R, Küppers J et al.. (2020) Cell-permeable high-affinity tracers for G_q proteins provide structural insights, reveal distinct binding kinetics and identify small molecule inhibitors.. Br J Pharmacol, 177 (8): (1898-1916). [PMID:31881095]
2. Adeosun SO et al.. (2018) A Novel Fluorescence-Based Assay for the Measurement of Biliverdin Reductase Activity.. React Oxyg Species (Apex), 5 (13): (35-45). [PMID:29379885]
3. Poser SW et al.. (2019) Controlling distinct signaling states in cultured cancer cells provides a new platform for drug discovery.. FASEB J, 33 (8): (9235-9249). [PMID:31145643]

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