Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
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. |
分子量 | 386.25 |
分子式 | C15H13Cl2N3O3S |
CAS No. | 2765077-82-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
FAAH/MAGL-IN-2 2765077-82-3 Inhibitor inhibitor inhibit