MAGLi 432
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease.
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- CAS No.: 2361575-20-2
- 화학식: C22H24BrClN2O2
- 분자량:463.80
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
MAGLi 432 (10 μΜ, 25 min) displays selectivity and potency for MAGL over other serine hydrolases in mouse and human brain lysates[1].
MAGLi 432 (1 μΜ, 6 h) inhibits MAGL activity and robustly enhances 2-AG levels in human NVU cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human BMECs (hCMEC/D3), primary human astrocytes, and pericytes
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Concentration:10 nM, 100 nM, 1 μM and 10 μM
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Incubation Time:6 h
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Result:Inhibited MAGL activity in a dose-dependent manner, and increased 2-AG levels in all cell types.
Modulated arachidonic acid levels in a cell specific-manner, with no effect in BMECs, but significant depletion in astrocytes and pericytes.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD-1 mice model of LPS-induced neuroinflammation[1]
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Dosage:1 mg/kg for 3 consecutive days
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Administration:Intraperitoneal injection
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Result:Accumulated ~10-fold more 2-AG than vehicle controls, reducted LPS-induced PGE2.
Increased LCN2 and TNF expression compared to the LPS treatment.
Chemical Information
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CAS No. 2361575-20-2
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분자량 463.80
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화학식 C22H24BrClN2O2
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SMILES
O=C(C1=CC=CC(OC)=C1Br)N2C[C@](CC[C@H](C3=CC=C(Cl)C=C3)C4)([H])N4CC2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MAGLi 432 Related Classifications
HY-150702 Related Classifications
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