M6766
Based on 1 Customer Validation
M6766 is a selective endoplasmic reticulum oxidoreductase 1α (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.
For research use only. We do not sell to patients.
- Purity : 99.43%
- CAS No.: 696628-90-7
- Formula: C19H16N6S
- Molecular Weight:360.44
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
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. Further protocols information, click here.
In Vivo
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.
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Animal Model:Thrombosis mice models induced by FeCl3-mediated injury[1]
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Dosage:0.3 μg/g
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Administration:Intravenously injection
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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.
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Animal Model:Mice models of ischemic stroke[1]
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Dosage:0.3 μg/g
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Administration:Intravenously injection
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Result:Decreased the Bederson score and increased grip strength.
Reduced infarct volume following focal brain ischemia.
Chemical Information
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CAS No. 696628-90-7
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Appearance Solid
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Molecular Weight 360.44
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Formula C19H16N6S
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Color Light yellow to yellow
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SMILES
CN1C(SC2=C3CCCCC3=C(C4=NC5=CC=CC=C5N42)C#N)=NN=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (277.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
Purity & Documentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7744 mL | 13.8719 mL | 27.7439 mL | 69.3597 mL |
| 5 mM | 0.5549 mL | 2.7744 mL | 5.5488 mL | 13.8719 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7744 mL | 6.9360 mL | |
| 15 mM | 0.1850 mL | 0.9248 mL | 1.8496 mL | 4.6240 mL | |
| 20 mM | 0.1387 mL | 0.6936 mL | 1.3872 mL | 3.4680 mL | |
| 25 mM | 0.1110 mL | 0.5549 mL | 1.1098 mL | 2.7744 mL | |
| 30 mM | 0.0925 mL | 0.4624 mL | 0.9248 mL | 2.3120 mL | |
| 40 mM | 0.0694 mL | 0.3468 mL | 0.6936 mL | 1.7340 mL | |
| 50 mM | 0.0555 mL | 0.2774 mL | 0.5549 mL | 1.3872 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4624 mL | 1.1560 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3468 mL | 0.8670 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2774 mL | 0.6936 mL |