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MK-2894

CAS No. : 1006036-87-8

MCE 国际站：MK-2894

产品活性：MK-2894 是一种有效的、选择性的、具有口服活性的高亲和力 (K_i=0.56 nM) 的前列腺素受体 4 (EP₄ receptor) 的拮抗剂 (IC₅₀=2.5 nM)。MK-2894 在动物疼痛/炎症模型中具有较强的抗炎活性，可用于关节炎的研究。

研究领域：GPCR/G Protein

作用靶点：Prostaglandin Receptor

In Vitro: 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.

In Vivo: 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 (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 (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 (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 (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.

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