2. Metabolic Enzyme/Protease
  3. MAGL
  4. MAGL-IN-4

MAGL-IN-4 

Cat. No.: HY-132310 Purity: 99.91%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

MAGL-IN-4 Chemical Structure

MAGL-IN-4 Chemical Structure

CAS No. : 2135785-20-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 539 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 539 In-stock
Solid
5 mg USD 490 In-stock
10 mg USD 820 In-stock
25 mg USD 1700 In-stock
50 mg USD 2650 In-stock
100 mg USD 4200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

364.82

Appearance

Solid

Formula

C18H21ClN2O4
CAS No.
SMILES

CC1=C(C=C(C=C1)COC2CN(C([[email protected]]3C[[email protected]]4(COC(N4)=O)C3)=O)C2)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
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 (274.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.91%

COA (247 KB) HNMR (137 KB) LCMS (259 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

MAGL-IN-42135785-20-3MAGLMonoacylglycerol lipasemonoacylglycerollipaseblood-brainbarrierBBBendocannabinoid2-AGFAAHABHD6CB1CB2hERGInhibitorinhibitorinhibit

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