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

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.

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M6766

M6766 Chemical Structure

CAS No. : 1432364-02-7

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Description

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)

In Vitro

M6766 (1-10 μM, 20 mins) inhibits FAD-enhanced ERO1α activity in a concentration-dependent manner[1].
M6766 (1-100 μM, 20 mins) does not inhibit the activities of H2O2, MAO-A and PDI[1].
M6766 (1-5 μM, 20 mins) inhibits P-selectin exposure (α-granule secretion) and αIIbβ3 integrin activation in platelets[1].
M6766 (1-5 μM, 20 mins) inhibits platelet aggregation and ATP secretion in platelets[1].
M6766 (5 μM, 20 mins) induces ROS production and increases annexin V binding in platelets[1].
M6766 (5 μM, 20 mins) inhibits CCL5 secretion from activated platelets in platelets[1].
M6766 (5 μM, 20 mins) reduces surface coverage and volume of platelet thrombi over collagen-coated surfaces[1].
M6766 (2-5 μM, 20 mins) inhibits both Ca2+ release and influx in activated platelets[1].
M6766 (5 μM, 20 mins) significantly reduces the interaction between ERO1α and STIM1 in platelets[1].

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

In Vivo

M6766 (0.3 μg/g, i,v.) attenuates platelet thrombus formation in arterial thrombosis mice[1].
M6766 (0.3 μg/g, i,v.) reduces brain damage in ischemic stroke mice[1].

MedChemExpress (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.
Molecular Weight

361.42

Formula

C18H15N7S

CAS No.
SMILES

CN1C(SC2=C3CCCCC3=C(C4=NC5=CC=CC=C5N42)C#N)=NN=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • 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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