| Bioactivity | 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]. |
| Target | IC50: 11 nM (FAAH); 36 nM (MAGL) |
| Invitro | FAAH/MAGL-IN-2 (compound 14) (1, 3, 10, 30, 100 μM) shows potent neuroprotection effect[1]. Cell Cytotoxicity Assay[1] Cell Line: |
| 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]. Pharmacokinetic parameters |
| Name | FAAH/MAGL-IN-2 |
| CAS | 2765077-82-3 |
| Formula | C15H13Cl2N3O3S |
| Molar Mass | 386.25 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Jaiswal S, et al. Synthesis and evaluation of dual fatty acid amide hydrolase-monoacylglycerol lipase inhibition and antinociceptive activities of 4-methylsulfonylaniline-derived semicarbazones. Bioorg Med Chem. 2022; 60:116698. |