1. Metabolic Enzyme/Protease
    Neuronal Signaling
  2. FAAH
    MAGL
  3. FAAH/MAGL-IN-2

FAAH/MAGL-IN-2 

Cat. No.: HY-143264
Handling Instructions

FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment.

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

FAAH/MAGL-IN-2 Chemical Structure

FAAH/MAGL-IN-2 Chemical Structure

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Description

FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment[1].

IC50 & Target

IC50: 11 nM (FAAH); 36 nM (MAGL)[1]

In Vitro

FAAH/MAGL-IN-2 (compound 14) (1, 3, 10, 30, 100 μM) shows potent neuroprotection effect[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 1, 3, 10, 30, 100 μM
Incubation Time: 24 h
Result: Showed potent neuroprotection effect.
In Vivo

FAAH/MAGL-IN-2 (10 mg/kg) has the potential to produce a significant anti-nociceptive effect without affecting of motor coordination and locomotor activity[1].
FAAH/MAGL-IN-2 (5, 10, 20 mg/kg) has the potential to treat neuropathic pain without causing locomotion impairment[1].
FAAH/MAGL-IN-2 (2000 mg/kg; p.o.; female rats) shows well tolerated and safe up to 2000 mg/kg in the oral dose and did not alter the liver enzymes activity[1].
FAAH/MAGL-IN-2 (20 mg/kg; p.o.) shows a good absorption behavior after oral administration[1].
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in 200–250 g, male Wistar rats[1].

200–250 g, male Wistar rats; 20 mg/kg; p.o.[1]
Pharmacokinetic parameters Results (Plasma)
Cmax (μg/mL) 22.04±2.5
Tmax (h) 0.5
AUC(0-t) (μg min/mL) 535±1.5
t1/2 (h) 20.58
MRT 0-inf (h) 0.5

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

Animal Model: Nerve-injured rats (CCI model)[1]
Dosage: 5, 10, 20 mg/kg
Administration:
Result: Significantly increased paw withdrawal threshold and attenuated tail flick latency in nerve injured rats.
Animal Model: 200–250 g, male Wistar rats[1]
Dosage: 20 mg/kg
Administration: Oral administration
Result: Showed a good absorption behavior after oral administration.
Molecular Weight

386.25

Formula

C15H13Cl2N3O3S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Product Name:
FAAH/MAGL-IN-2
Cat. No.:
HY-143264
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