1. Anti-infection Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Endoplasmic Reticulum Oxidoreductase 1 (ERO1) Reactive Oxygen Species (ROS)
  3. M6766

M6766 是一种选择性内质网氧化还原酶 1α (ERO1α) 抑制剂,其 IC50 值为 1.4 μM,KD 值为 1.1 μM。M6766 对 ERO1β 也有抑制作用,其 IC50 值为 7.2 μM。M6766 与 ERO1α 中的黄素腺嘌呤二核苷酸结合口袋结合。M6766 可抑制颗粒分泌、αIIbβ3 整合素激活、Ca2+ 动员和血小板聚集。M6766 可用于神经系统疾病的研究,如缺血性卒中。

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M6766

M6766 Chemical Structure

CAS No. : 1432364-02-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

M6766 is a selective endoplasmic reticulum oxidoreductase (ERO1α) inhibitor with an IC50 of 1.4 μM and a KD of 1.1 μM. M6766 also inhibits ERO1β with an IC50 of 7.2 μM. M6766 binds to the flavin adenine dinucleotide-binding pocket in ERO1α. M6766 inhibits granule secretion, αIIbβ3 integrin activation, Ca2+ mobilization, and platelet aggregation. M6766 can be used for the research of neurological disease, such as ischemic stroke[1].

IC50 & Target[1]

ERO1α

1.4 μM (IC50)

ERO1α

1.1 μM (Kd)

体外研究
(In Vitro)

M6766 (1-10 μM, 20 mins) 以浓度依赖性的方式抑制 FAD 增强的 ERO1α 活性[1]
M6766 (1-100 μM, 20 mins) 不抑制 H₂O₂、MAO-A 和 PDI 的活性[1]
M6766 (1-5 μM, 20 mins) 抑制血小板中 P-选择素的暴露 (α 颗粒分泌) 和 αIIbβ3 整合素的激活[1]
M6766 (1-5 μM, 20 mins) 抑制血小板中的血小板聚集和 ATP 分泌[1]
M6766 (5 μM, 20 mins) 诱导血小板中活性氧的产生并增加膜联蛋白 V 的结合[1]
M6766 (5 μM, 20 mins) 抑制活化血小板中 CCL5 的分泌[1]
M6766 (5 μM, 20 mins) 减少胶原蛋白包被表面上血小板血栓的表面覆盖率和体积[1]
M6766 (2-5 μM, 20 mins) 抑制活化血小板中 Ca2+ 的释放和内流[1]
M6766 (5 μM, 20 mins) 可显著减少血小板中 ERO1α 与 STIM1 之间的相互作用[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

M6766 (0.3 μg/g,静脉注射) 可减轻动脉血栓形成小鼠中的血小板血栓形成[1]
M6766 (0.3 μg/g,静脉注射) 可减轻缺血性中风小鼠的脑损伤[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Thrombosis mice models induced by FeCl3-mediated injury[1]
Dosage: 0.3 μg/g
Administration: Intravenously injection
Result: Significantly prolonged the time to occlusion (TTO) following 7% FeCl3.
Did not affect TTO after 10% FeCl3 application.
Did not prolong tail bleeding times or increase blood loss.
Animal Model: Mice models of ischemic stroke[1]
Dosage: 0.3 μg/g
Administration: Intravenously injection
Result: Decreased the Bederson score and increased grip strength.
Reduced infarct volume following focal brain ischemia.
分子量

361.42

Formula

C18H15N7S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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M6766
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HY-175593
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