PK150|cas:2165324-62-7|西域试剂

PK150,99.37%

产品编号：Bellancom-133119| CAS NO：2165324-62-7| 分子式：C₁₅H₈ClF₅N₂O₃| 分子量：394.68

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-133119	￥1500.00	杭州北京（现货）
Bellancom-133119	￥2500.00	杭州北京（现货）
Bellancom-133119	￥7500.00	杭州北京（现货）
Bellancom-133119	￥12500.00	杭州北京（现货）

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PK150

产品介绍

PK150 是一种 Sorafenib 的类似物。PK150 具有口服活性，具有抗菌活性。PK150 抑制甲氧西林敏感金黄色葡萄球菌 (MSSA)，耐甲氧西林金黄色葡萄球菌 (MRSA)，万古霉素中介金黄色葡萄球菌 (VISA) 的 MIC 分别为 0.3，0.3-1，0.3 µM。

生物活性

PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 µM, respectively.

体外研究

体内研究

The in vivo efficacy of PK150 against methicillin-sensitive S. aureus (MSSA) (strain SH1000) is demonstrated in a murine bloodstream infection model. PK150 (20 mg/kg; p.o.) significantly reduces bacterial loads in the liver and heart.
PK150 (10 and 20mg/kg orally; or 10mg/kg intravenously) shows no obvious signs of toxicity in mice. Higher i.v. dosing of 20mg/kg results in severe toxic effects and is thus avoided for subsequent therapeutic models.

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

Animal Model:	Pathogen-free 9-week old female C57BL/6J mice
Dosage:	20 mg/kg
Administration:	Administered p.o.
Result:	Bacterial loads in the liver and heart were both significantly reduced by approximately 100-fold.

Animal Model:	Outbred male CD-1 mice, 4 weeks old
Dosage:	10 and 20 mg/kg (Pharmacokinetic Analysis)
Administration:	Administered by intragastric gavage at 10 and 20 mg/kg or intravenously at 10 mg/kg
Result:	Oral bioavailability was approximately 63% and the mean residence time was slightly enhanced via this administration route. T_1/2=11.69±1.5, 9.67±0.2, and 9.37±0.5 hours for 10 mg/kg i.v., 10 mg/kg p.o., and 20 mg/kg p.o., respectively.

体内研究

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

Animal Model:	Pathogen-free 9-week old female C57BL/6J mice
Dosage:	20 mg/kg
Administration:	Administered p.o.
Result:	Bacterial loads in the liver and heart were both significantly reduced by approximately 100-fold.

Animal Model:	Outbred male CD-1 mice, 4 weeks old
Dosage:	10 and 20 mg/kg (Pharmacokinetic Analysis)
Administration:	Administered by intragastric gavage at 10 and 20 mg/kg or intravenously at 10 mg/kg
Result:	Oral bioavailability was approximately 63% and the mean residence time was slightly enhanced via this administration route. T_1/2=11.69±1.5, 9.67±0.2, and 9.37±0.5 hours for 10 mg/kg i.v., 10 mg/kg p.o., and 20 mg/kg p.o., respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (633.42 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5337 mL	12.6685 mL	25.3370 mL
5 mM	0.5067 mL	2.5337 mL	5.0674 mL
10 mM	0.2534 mL	1.2668 mL	2.5337 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: ≥ 2.08 mg/mL (5.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.27 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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% corn oil
Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.27 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。