FAAH/MAGL-IN-2,2765077-82-3

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FAAH/MAGL-IN-2

CAS No. : 2765077-82-3

MCE 国际站：FAAH/MAGL-IN-2

产品活性：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>K_i 值分别为 28 nM 和 60 nM)。FAAH/MAGL-IN-2 有研究神经性疼痛的潜力而不引起运动障碍。

研究领域：Metabolic Enzyme/Protease  |  Neuronal Signaling

作用靶点：FAAH  |  MAGL

In Vitro: FAAH/MAGL-IN-2 (compound 14) (1, 3, 10, 30, 100 μM) shows 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.
FAAH/MAGL-IN-2 (5, 10, 20 mg/kg) has the potential to treat neuropathic pain without causing locomotion impairment.
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.
FAAH/MAGL-IN-2 (20 mg/kg; p.o.) shows a good absorption behavior after oral administration.
Pharmacokinetic Parameters of JAK1/TYK2-IN-2 in 200–250 g, male Wistar rats.

200–250 g, male Wistar rats; 20 mg/kg; p.o.

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

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