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S81626

MK-2894

源叶(MedMol) 97%
  • 英文名:
  • MK-2894
  • 别名:
  • 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid; CS-0679; 4-[1-[[2,5-dimethyl-4-[[4-(trifluoromethyl)phenyl]methyl]thiophene-3-carbonyl]amino]cyclo
  • CAS号:
  • 1006036-87-8
  • 分子式:
  • C25H22F3NO3S
  • 分子量:
  • 473.51
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81626-5mg 97% ¥2400.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S81626-10mg 97% ¥4200.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: MK-2894 is a potent, selective, orally active and high affinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis
  • 靶点: Others
  • 体内研究:
    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 (Vdss=7.6 L/kg), good elimination half-lives (T1/2=15 h) and the maximum concentration reached (Cmax=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 (Vdss=2.6 L/kg), good elimination half-lives (T1/2=4.5 h) and the maximum concentration reached (Cmax=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 (Vdss=0.91 L/kg), good elimination half-lives (T1/2=8.8 h) and the maximum concentration reached (Cmax=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 se
  • 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, O'Neill G, Ducharme Y, Friesen R. The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluorometh 2. Tijana Markovič, et al. Structural features of subtype-selective EP receptor modulators. Drug Discov Today. 2017 Jan;22(1):57-71.
  • 溶解性: Soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 2.112 ml 10.559 ml 21.119 ml
    5 mM 0.422 ml 2.112 ml 4.224 ml
    10 mM 0.211 ml 1.056 ml 2.112 ml
    50 mM 0.042 ml 0.211 ml 0.422 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)


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