产品
编 号：F003121
分子式：C25H22F3NO3S
分子量：473.51
分子式：C25H22F3NO3S
分子量：473.51
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1006036-87-8
产品详情
生物活性：
MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis.
体内研究：
MK-2894 (oral administration, 20 mg/kg; intravenous?injection, 5 mg/kg) exhibits a favorable pharmacokinetic profile in mice, the moderate bioavailability F=21%, and slow to moderate clearance rate (CL=23 mL/min/kg), the volume of distribution (Vdss=7.6 L/kg), good elimination half-lives (T1/2=15 h) and the maximum concentration reached (Cmax=1.4 μM) in mice.MK-2894 (oral administration, 20 mg/kg; intravenous?injection, 5 mg/kg) exhibits a favorable pharmacokinetic profile in SD-rats, the moderate bioavailability F=29%, and slow to moderate clearance rate (CL=9.2 mL/min/kg), the volume of distribution (Vdss=2.6 L/kg), good elimination half-lives (T1/2=4.5 h) and the maximum concentration reached (Cmax=4.5 μM) in mice.MK-2894 (oral administration, 5 mg/kg; intravenous?injection, 1 mg/kg) exhibits a favorable pharmacokinetic profile in dogs, the moderate bioavailability F=32%, and slow to moderate clearance rate (CL=23 mL/min/kg), the volume of distribution (Vdss=0.91 L/kg), good elimination half-lives (T1/2=8.8 h) and the maximum concentration reached (Cmax=3.3 μM) in mice.MK-2894 (oral administration; 0.1 mg/kg-10 mg/kg; single dose) inhibits the acute carrageenan-induced mechanical hyperalgesia model in SD rats in a dose-dependent manner, it displays a inhibition of pain response when measured at 3 h post subplantar injection of carrageenan.MK-2894 (oral administration; 0.1 mg/kg-10 mg/kg;5 days) exhibits potent activity in inhibiting chronic paw swelling, in both the primary paw and the secondary paw, in a dose-dependent manner, the ED50 value is 0.02 mg/kg/day. The complete inhibition of the secondary paw swelling is at an ED100 of 0.1 mg/kg/day with a plasma concentration of 4 nM at 24 h after the final dose in an adjuvant-induced arthritis rat model.
体外研究：
MK-2894 shows inhibitory effects on PGE2-induced cAMP accumulation, the EP4 functional potency in HEK 293 and HWB cells with IC50 values of 2.5 nM and 11 nM, respectively.
MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis.
体内研究：
MK-2894 (oral administration, 20 mg/kg; intravenous?injection, 5 mg/kg) exhibits a favorable pharmacokinetic profile in mice, the moderate bioavailability F=21%, and slow to moderate clearance rate (CL=23 mL/min/kg), the volume of distribution (Vdss=7.6 L/kg), good elimination half-lives (T1/2=15 h) and the maximum concentration reached (Cmax=1.4 μM) in mice.MK-2894 (oral administration, 20 mg/kg; intravenous?injection, 5 mg/kg) exhibits a favorable pharmacokinetic profile in SD-rats, the moderate bioavailability F=29%, and slow to moderate clearance rate (CL=9.2 mL/min/kg), the volume of distribution (Vdss=2.6 L/kg), good elimination half-lives (T1/2=4.5 h) and the maximum concentration reached (Cmax=4.5 μM) in mice.MK-2894 (oral administration, 5 mg/kg; intravenous?injection, 1 mg/kg) exhibits a favorable pharmacokinetic profile in dogs, the moderate bioavailability F=32%, and slow to moderate clearance rate (CL=23 mL/min/kg), the volume of distribution (Vdss=0.91 L/kg), good elimination half-lives (T1/2=8.8 h) and the maximum concentration reached (Cmax=3.3 μM) in mice.MK-2894 (oral administration; 0.1 mg/kg-10 mg/kg; single dose) inhibits the acute carrageenan-induced mechanical hyperalgesia model in SD rats in a dose-dependent manner, it displays a inhibition of pain response when measured at 3 h post subplantar injection of carrageenan.MK-2894 (oral administration; 0.1 mg/kg-10 mg/kg;5 days) exhibits potent activity in inhibiting chronic paw swelling, in both the primary paw and the secondary paw, in a dose-dependent manner, the ED50 value is 0.02 mg/kg/day. The complete inhibition of the secondary paw swelling is at an ED100 of 0.1 mg/kg/day with a plasma concentration of 4 nM at 24 h after the final dose in an adjuvant-induced arthritis rat model.
体外研究：
MK-2894 shows inhibitory effects on PGE2-induced cAMP accumulation, the EP4 functional potency in HEK 293 and HWB cells with IC50 values of 2.5 nM and 11 nM, respectively.
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