FAAH/MAGL-IN-2

Name: FAAH/MAGL-IN-2
Brand: TargetMol
SKU: T61707
Rating: 4.5 (1 reviews)

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产品编号 T61707Cas号 2765077-82-3

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 有研究神经性疼痛的潜力而不引起运动障碍。

FAAH/MAGL-IN-2

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产品编号 T61707Cas号 2765077-82-3

规格	价格	库存
25 mg	¥ 10,600	10-14周
50 mg	¥ 13,800	10-14周
100 mg	¥ 17,500	10-14周

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产品描述	FAAH/MAGL-IN-2, a potent and reversible inhibitor of FAAH and MAGL, demonstrates oral activity and the ability to cross the blood-brain barrier. It exhibits IC50 values of 11 nM for FAAH and 36 nM for MAGL (Ki values of 28 nM and 60 nM, respectively). This compound shows promise for neuropathic pain research, without impairing locomotion [1].
体外活性	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.
体内活性	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.