产品
编 号：F070943
分子式：C24H20ClN5O3
分子量：461.9
分子式：C24H20ClN5O3
分子量：461.9
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1207253-08-4
产品详情
生物活性：
MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia.
体内研究：
MK-1064 (30?mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice.MK-1064 (30?mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats.MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey.Animal Model:Wild-type and OX2R knockout mice
Dosage:30 mg/kg
Administration:Oral administration
Result:Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5?hours following treatment.
Animal Model:Rat, dog, and rhesus monkey (Pharmacokinetics assay)
Dosage:1, 2, 3, 5 mg/kg
Administration:Oral administration (P.O.), intravenous injection (I.V.)
Result:Pharmacokinetics profile of MK-1064.SpeciesDose (mg/kg) CL (mL/min/kg) t1/2 (h) Dose (mg/kg)Cmax (μM)F (%)
Rat2 (I.V.)390.35 (P.O.)1.554
Dog1 (I.V.)161.03 (P.O.)1.048
Rhesus2 (I.V.)120.85 (P.O.)0.916
MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia.
体内研究：
MK-1064 (30?mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice.MK-1064 (30?mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats.MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey.Animal Model:Wild-type and OX2R knockout mice
Dosage:30 mg/kg
Administration:Oral administration
Result:Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5?hours following treatment.
Animal Model:Rat, dog, and rhesus monkey (Pharmacokinetics assay)
Dosage:1, 2, 3, 5 mg/kg
Administration:Oral administration (P.O.), intravenous injection (I.V.)
Result:Pharmacokinetics profile of MK-1064.SpeciesDose (mg/kg) CL (mL/min/kg) t1/2 (h) Dose (mg/kg)Cmax (μM)F (%)
Rat2 (I.V.)390.35 (P.O.)1.554
Dog1 (I.V.)161.03 (P.O.)1.048
Rhesus2 (I.V.)120.85 (P.O.)0.916
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