MK-2894|cas:1006036-87-8|西域试剂

MK-2894,99.31%

产品编号：Bellancom-10413| CAS NO：1006036-87-8| 分子式：C₂₅H₂₂F₃NO₃S| 分子量：473.51

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-10413	￥1674.00	杭州北京（现货）
Bellancom-10413	￥2864.00	杭州北京（现货）
Bellancom-10413	￥10044.00	杭州北京（现货）

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MK-2894

产品介绍

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。

生物活性

MK-2894 is a potent, selective, orally active and high affinity (K_i=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.

体外研究

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.

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

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 (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.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (105.59 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1119 mL	10.5594 mL	21.1189 mL
5 mM	0.4224 mL	2.1119 mL	4.2238 mL
10 mM	0.2112 mL	1.0559 mL	2.1119 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.28 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.28 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.28 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。