PF-04802367 PF-367|cas:1962178-27-3|西域试剂

PF-04802367 PF-367,98.84%

产品编号：Bellancom-122026| CAS NO：1962178-27-3| 分子式：C₁₆H₁₆ClN₅O₃| 分子量：361.78

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货号	价格	库存与货期
Bellancom-122026	￥3800.00	杭州北京（现货）
Bellancom-122026	￥6000.00	杭州北京（现货）
Bellancom-122026	￥11500.00	杭州北京（现货）

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PF-04802367 PF-367

产品介绍

PF-04802367 (PF-367) 是一种高选择性 GSK-3 抑制剂，对 GSK-3β 酶的 IC₅₀ 为 2.1 nM。PF-04802367 具有理想的中枢神经系统 (CNS) 特性和效力。PF-04802367 抑制两种 GSK-3 亚型（GSK-3α 和 GSK-3β）效果差不多， IC₅₀ 值分别为 10.0 和 9.0 nM。

生物活性

PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC₅₀ of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC₅₀ values of 10.0 and 9.0 nM in mobility shift assays, respectively.

体外研究

PF-04802367 (PF-367) is efficient at inhibiting GSK-3β enzymatic activity in vitro with ligand and lipophilic efficiency scores of 0.46 and 7.0, respectively.
PF-367 has reasonable in vitro stability in human hepatic microsomes (t_1/2=78.7 min), has excellent passive permeability.
In a stable inducible CHO cell line over-expressing GSK-3β and its substrate tau, PF-367 inhibited phosphorylation of tau with an IC₅₀ of 466 nM.
PF-367 has good cell viability (IC₅₀ of 117 μM in THLE cytotoxicity assays) and an IC₅₀ >100 μM in a hERG screening assay.
PF-367 shows significant right shifts against β-catenin translocation in HeLa cells with EC₅₀ of 6.2 μM, gene transcription in U20S cells with EC₅₀ of 20.6 μM, and cell proliferation in HeLa cells as evaluated by Ki-67 incorporation with EC₅₀ of 9.0 μM.

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

体内研究

PF-04802367 (PF-367) a potent GSK-3 inhibitor with exceptional kinome selectivity that modulates phosphorylated tau levels in vivo. Inhibition of phosphorylation of tau in brain by PF-367 (A single subcutaneous of 1, 3.2, 10, 32 or 50 mg/kg) is dose-dependent.
PF-04802367 (PF-367), a potent type-I dual GSK-3α/β inhibitor, showing promising absorption; distribution, metabolism and elimination (ADME) properties combined with robust CNS/peripheral p-Tau and muscle phosphorylated glycogen synthase (pGS) inhibition in vivo.

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

Animal Model:	Sprague-Dawley rats
Dosage:	1, 3.2, 10, 32 or 50 mg/kg
Administration:	A single subcutaneous
Result:	Inhibition of phosphorylation of tau in brain is dose-dependent.

体内研究

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

Animal Model:	Sprague-Dawley rats
Dosage:	1, 3.2, 10, 32 or 50 mg/kg
Administration:	A single subcutaneous
Result:	Inhibition of phosphorylation of tau in brain is dose-dependent.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (276.41 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7641 mL	13.8206 mL	27.6411 mL
5 mM	0.5528 mL	2.7641 mL	5.5282 mL
10 mM	0.2764 mL	1.3821 mL	2.7641 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 (6.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.91 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 (6.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.91 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 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 (6.91 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.91 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。