MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

MK-2894 sodium salt

CAS No. : 1006036-88-9

MCE 站：MK-2894 sodium salt

产品活性：MK-2894 sodium salt 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 sodium salt 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 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 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.

相关产品：Prostaglandin E2  |  Prostaglandin E1  |  Iloprost  |  PF-04418948  |  Tranilast  |  ONO-AE3-208  |  AH 6809  |  U-46619  |  Latanoprost  |  Laropiprant  |  Rebamipide  |  Travoprost  |  RO1138452  |  Ramatroban  |  p-Hydroxycinnamic acid  |  Bimatoprost  |  Pectolinarin  |  Taprenepag  |  Dinoprost tromethamine salt  |  (+)-Cloprostenol  |  Dazoxiben  |  Evatanepag  |  L-798106  |  Seratrodast  |  Nedocromil  |  Treprostinil  |  CAY10471 Racemate  |  Cloprostenol sodium salt  |  L 888607  |  AZ12672857

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。