产品
编 号：F755752
分子式：C15H13Cl2N3O3S
分子量：386.25
分子式：C15H13Cl2N3O3S
分子量：386.25
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CAS No: 2765077-82-3
产品详情
生物活性：
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 research neuropathic pain without causing locomotion impairment.
体内研究：
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.Pharmacokinetic parametersResults (Plasma)
200–250 g, male Wistar rats; 20 mg/kg; p.o.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
Animal Model:Nerve-injured rats (CCI model)
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
Dosage:20 mg/kg
Administration:Oral administration
Result:Showed a good absorption behavior after oral administration.
体外研究：
FAAH/MAGL-IN-2 (compound 14) (1, 3, 10, 30, 100 μM) shows potent neuroprotection effect.
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 research neuropathic pain without causing locomotion impairment.
体内研究：
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.Pharmacokinetic parametersResults (Plasma)
200–250 g, male Wistar rats; 20 mg/kg; p.o.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
Animal Model:Nerve-injured rats (CCI model)
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
Dosage:20 mg/kg
Administration:Oral administration
Result:Showed a good absorption behavior after oral administration.
体外研究：
FAAH/MAGL-IN-2 (compound 14) (1, 3, 10, 30, 100 μM) shows potent neuroprotection effect.
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