[CAS NO. 2135785-20-3] MAGL-IN-4
PRODUCTS SPECIFICATIONS [2135785-20-3]
DESCRIPTION [2135785-20-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 364.82 |
| Molecular Formula | C18H21ClN2O4 |
| SMILES | CC1=C(C=C(C=C1)COC2CN(C([C@H]3C[C@]4(COC(N4)=O)C3)=O)C2)Cl |
Summary
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC 50 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 IC
50
>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.
Appearance
Solid
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
DMSO : 100 mg/mL ( 274.11 mM ; Need ultrasonic)
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 |