FAAH/MAGL-IN-2 是一种有效的，可逆的，具有口服活性且可透过血脑屏障的FAAH和MAGL抑制剂，其IC50值分别为 11 nM 和 36 nM (b>Ki值分别为 28 nM 和 60 nM)。FAAH/MAGL-IN-2 有治疗神经性疼痛的潜力而不引起运动障碍。

FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC 50 s of 11 nM and 36 nM ( K i s of 28 nM and 60 nM), respectively. FAAH/MAGL-IN-2 has the potential to treat neuropathic pain without causing locomotion impairment [1].

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

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

C15H13Cl2N3O3S

386.25

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years