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Art. -Nr.: HY-150702

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2361575-20-2
Formel: C₂₂H₂₄BrClN₂O₂
Molecular Weight:463.80

Speicherung:

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

Data Sheet (269 KB)

MAGLi 432 Chemical Structure

CAS. Nr.: 2361575-20-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

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.

Western Blot Analysis^[1]

Cell Line:

Human BMECs (hCMEC/D3), primary human astrocytes, and pericytes
Concentration:

10 nM, 100 nM, 1 μM and 10 μM
Incubation Time:

6 h
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.

In Vivo

MAGLi 432 (intraperitoneal injection, 1 mg/kg for 3 consecutive days) inhibits MAGL in the brain and reduces arachidonic acid and PGE₂ levels in LPS-induced neuroinflammation, without reducing BBB permeability and inflammatory cytokine expression in the cortex^[1].

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

Animal Model:

Male CD-1 mice model of LPS-induced neuroinflammation^[1]
Dosage:

1 mg/kg for 3 consecutive days
Administration:

Intraperitoneal injection
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

CAS. Nr. 2361575-20-2
Molecular Weight 463.80
Formel C₂₂H₂₄BrClN₂O₂
SMILES

O=C(C1=CC=CC(OC)=C1Br)N2C[C@](CC[C@H](C3=CC=C(Cl)C=C3)C4)([H])N4CC2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Alicia Kemble, et al. A potent and selective inhibitor for the modulation of MAGL activity in the neurovasculature. bioRxiv 2022.05.04.490688.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

MOQ

Minimum order quantity

100 mg

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