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MAGL-IN-4

Catalog No. T9687 CAS 2135785-20-3

Synonyms: His121 ARG57

MAGL-IN-4 is one of the monoacylglycerol Lipase (MAGL) inhibitors in central nervous system-related diseases.

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MAGL-IN-4, CAS 2135785-20-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	MAGL-IN-4 is one of the monoacylglycerol lipase (MAGL) inhibitors in central nervous system-related diseases.
Targets&IC50	MAGL:6.2 nM
In vitro	MAGL-IN-4 showed potent in vitro MAGL inhibitory activity (IC50 6.2 nM), good oral absorption and blood-brain barrier penetration[1].
In vivo	MAGL-IN-4 showed significant pharmacodynamic changes (2-arachidonoylglycerol increase and arachidonic acid decrease) at 0.3-10 mg/kg, po. in mice[1].

Synonyms	His121 ARG57
Molecular Weight	364.82
Formula	C18H21ClN2O4
CAS No.	2135785-20-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 88 mg/mL (241.21 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Shuhei Ikeda, et al. Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H-benzo[ b][1,4]oxazin-6-yl Moiety. J Med Chem. 2021 Aug 12;64(15):11014-11044.

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

MAGL-IN-4 2135785-20-3 Metabolism Lipase Monoacylglycerol lipase CB1 lipase monoacylglycerol CB2 Inhibitor inhibit BBB barrier MAGLIN4 MAGL IN 4 blood-brain endocannabinoid His121 ARG57 hERG FAAH 2-AG ABHD6 MAGL inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.