1. Metabolic Enzyme/Protease
  2. MAGL
  3. MAGL-IN-1

MAGL-IN-1 

Cat. No.: HY-111538 Purity: 99.90%
Handling Instructions

MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays.

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

MAGL-IN-1 Chemical Structure

MAGL-IN-1 Chemical Structure

CAS No. : 2324160-91-8

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Description

MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays[1].

IC50 & Target

IC50: 80 nM (MAGL)[1]

In Vitro

MAGL-IN-1 (compound 23) (0.02-200 μM; 96 h) produces an appreciable inhibition of cell viability in all the tested cancer cell lines, with IC50s ranging from 7.9 to 57 μM[1].
MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a Ki of 39 nM[1].
MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM[1].
MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [3H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC50 of 193 nM[1].
MAGL-IN-1 (0.01-30 μM; 15 min) inhibits 2-OG hydrolysis in a concentration-dependent manner in mouse brain membrane preparations, with an IC50 of 2.1 μM[1].

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

Cell Proliferation Assay[1]

Cell Line: HCT116, MDA-MB-231, CAOV3, OVCAR3, SKOV3, and MRC5 cells
Concentration: 0.02-200 μM
Incubation Time: 96 hours
Result: Inhibited the growth of human breast MDA-MB-231, colorectal HCT116, and ovarian CAOV3, OVCAR3, and SKOV3 cancer cells, with IC50s of 7.9, 21, 25, 57, and 15 μM, respectively.
Was inactive against MRC5 (IC50>100 μM).
In Vivo

MAGL (compound 23) (50 mg/kg; a single i.p.) increases the 2-AG level in plasma and brain, and does not alter anandamide (AEA), arachidonic acid and prostaglandin levels in plasma and brain of mice[1].

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

Animal Model: Male C57BL6 mice, 8-10 weeks old[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; once
Result: Increased 2-AG levels in the brain and plasma.
Molecular Weight

369.43

Formula

C₂₂H₂₄FNO₃

CAS No.

2324160-91-8

SMILES

O=C(C1CCN(C(C2=CC(O)=CC=C2F)=O)CC1)C3=CC=C(C(C)C)C=C3

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 : 62.5 mg/mL (169.18 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7069 mL 13.5344 mL 27.0687 mL
5 mM 0.5414 mL 2.7069 mL 5.4137 mL
10 mM 0.2707 mL 1.3534 mL 2.7069 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: 2.08 mg/mL (5.63 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

MAGL-IN-1MAGLMonoacylglycerol lipaseanti-proliferativebreastcolorectalovariancancermonoacylglycerollipaseInhibitorinhibitorinhibit

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