MK-2894 sodium salt

MK-2894 sodium salt is a potent, selective, orally active and high affinity ( K i =0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) ( IC 50 =2.5 nM). MK-2894 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis. In Vivo MK-2894 sodium salt (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 (V dss =7.6 L/kg), good elimination half-lives (T 1/2 =15 h) and the maximum concentration reached (C max =1.4 μM) in mice . MK-2894 sodium salt (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 (V dss =2.6 L/kg), good elimination half-lives (T 1/2 =4.5 h) and the maximum concentration reached (C max =4.5 μM) in mice . MK-2894 sodium salt (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 (V dss =0.91 L/kg), good elimination half-lives (T 1/2 =8.8 h) and the maximum concentration reached (C max =3.3 μM) in mice . MK-2894 sodium salt (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 sodium salt (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 ED 50 value is 0.02 mg/kg/day. The complete inhibition of the secondary paw swelling is at an ED 100 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet