PF-3644022|cas:1276121-88-0|西域试剂

PF-3644022,99.93%

产品编号：Bellancom-107427| CAS NO：1276121-88-0| 分子式：C₂₁H₁₈N₄OS| 分子量：374.46

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货号	价格	库存与货期
Bellancom-107427	￥3600.00	杭州北京（现货）
Bellancom-107427	￥5700.00	杭州北京（现货）
Bellancom-107427	￥11500.00	杭州北京（现货）

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PF-3644022

产品介绍

PF-3644022 是一种有效的，选择性的，口服活性的，具有 ATP 竞争性的 MAPKAPK2 (MK2) 抑制剂，IC₅₀ 为 5.2 nM，K_i 为 3 nM。PF-3644022 还抑制 MK3 和 p38 调节/激活激酶 (PRAK)，IC₅₀ 分别为 53 nM 和 5.0 nM。PF-3644022 有效抑制 TNFα 的产生并具有抗炎作用。

生物活性

PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC₅₀ of 5.2 nM and a K_i of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC₅₀s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.

体外研究

The inhibitory activity of PF-3644022 against other MAPKAP kinase family members is evaluated. Other than MNK2 with an IC₅₀ of 148 nM, other family members are largely not inhibited, showing at least several hundred-fold selectivity versus MK2.
In the human U937 monocytic cell line or peripheral blood mononuclear cells, PF-3644022 potently inhibits TNFα production with similar activity (IC₅₀ of 160 nM). PF-3644022 blocks TNFα and IL-6 production in LPS-stimulated human whole blood with IC₅₀ values of 1.6 and 10.3 μM, respectively. Inhibition of TNFα in U937 cells and blood correlates closely with inhibition of phospho-heat shock protein 27, a target biomarker of MK2 activity.

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

体内研究

PF-3644022 (3-100 mg/kg; oral gavage; twice a day; for 12 days; Lewis rats) treatment shows dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing, with ED₅₀ value of 20 mg/kg.

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

Animal Model:	Female Lewis rats (125-140 g) injected with streptococcal cell wall
Dosage:	3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg
Administration:	Oral gavage; twice a day; for 12 days
Result:	Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.

体内研究

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

Animal Model:	Female Lewis rats (125-140 g) injected with streptococcal cell wall
Dosage:	3 mg/kg, 10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg
Administration:	Oral gavage; twice a day; for 12 days
Result:	Showed dose-dependent inhibition of chronic paw swelling measured on day 21 after 12 days of oral dosing.

性状

Solid

溶解性数据

In Vitro:

DMSO : 41.67 mg/mL (111.28 mM; ultrasonic and warming and heat to 80°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6705 mL	13.3526 mL	26.7051 mL
5 mM	0.5341 mL	2.6705 mL	5.3410 mL
10 mM	0.2671 mL	1.3353 mL	2.6705 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 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (5.55 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (5.55 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 20.8 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