生物活性 |
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.
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体内研究(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;
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储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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参考文献 |
[1]. Blouin M, Han Y, Burch J, Farand J, Mellon C, Gaudreault M, Wrona M, Lévesque JF, Denis D, Mathieu MC, Stocco R, Vigneault E, Therien A, Clark P, Rowland S, Xu D, ONeill G, Ducharme Y, Friesen R. The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluorometh[2]. Tijana Markovi?, et al. Structural features of subtype-selective EP receptor modulators. Drug Discov Today. 2017 Jan;22(1):57-71.
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