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MAGL-IN-4

Catalog No.GC63055

MAGL-IN-4는 6.2nM의 IC50을 갖는 경구 활성, 선택적 및 가역적 모노아실글리세롤 리파제(MAGL) 억제제입니다.

Products are for research use only. Not for human use. We do not sell to patients.

MAGL-IN-4 Chemical Structure

Cas No.: 2135785-20-3

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$303.00
재고 있음
1mg
US$158.00
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5mg
US$378.00
재고 있음
10mg
US$527.00
재고 있음

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고객 리뷰

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Sample solution is provided at 25 µL, 10mM.

Description of MAGL-IN-4

MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain[1].

MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL[1]. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA)[1].

MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice[1].

[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.

Chemical Properties of MAGL-IN-4

Cas No. 2135785-20-3 SDF
Formula C18H21ClN2O4 M.Wt 364.82
Solubility DMSO : 100 mg/mL (274.11 mM; Need ultrasonic) Storage
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of MAGL-IN-4

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.7411 mL 13.7054 mL 27.4108 mL
5 mM 0.5482 mL 2.7411 mL 5.4822 mL
10 mM 0.2741 mL 1.3705 mL 2.7411 mL
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In vivo Formulation Calculator (Clear solution) of MAGL-IN-4

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 14 reference(s) in Google Scholar.)

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