| 中文名称 |
MK-2894 sodium salt
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| 中文别名 |
4-[1-[[[2,5-二甲基-4-[[4-(三氟甲基)苯基]甲基]-3-噻吩基]羰基]氨基]环丙基]苯甲酸钠盐;MK-2894 钠盐
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| 英文名称 |
MK-2894 sodium salt
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| 英文别名 |
1-Cyclopentene-1-heptanoic acid, 5-oxo-3-[(triethylsilyl)oxy]-, Methyl ester;MK-2894 (sodium salt);sodium,4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclopropyl]benzoate;MK 2894 (sodium salt);4-[1-[[[2,5-Dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]-3-thienyl]carbonyl]amino]cyclopropyl]benzoic acid sodium salt;MK-2894 Sodium;MK-2894 Na salt;MK-2894 sodium salt
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| Cas No. |
1006036-88-9
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| 分子式 |
C25H21NO3F3S-.Na+
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| 分子量 |
495.49
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| 包装储存 |
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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| 详情描述 |
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 (Ki=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。
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| 产品详情 |
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 (Ki=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。
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| 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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| 性状 |
Solid
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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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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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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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[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.
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。