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  3. MK-2894 sodium salt

MK-2894 sodium salt 

目录号: HY-10414 纯度: 98.09%
产品使用指南

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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MK-2894 sodium salt Chemical Structure

MK-2894 sodium salt Chemical Structure

CAS No. : 1006036-88-9

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5 mg ¥1674
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10 mg ¥2864
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50 mg ¥10044
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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MK-2894 sodium salt 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 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis[1][2].

IC50 & Target[1]

EP4

0.56 nM (Ki)

EP4

2.5 nM (IC50)

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 (Vdss=7.6 L/kg), good elimination half-lives (T1/2=15 h) and the maximum concentration reached (Cmax=1.4 μM) in mice[1].
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 (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[1].
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 (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[1].
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[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

495.49

Formula

C25H21F3NNaO3S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
MK-2894 sodium salt
目录号:
HY-10414
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