货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T28940-1ml	10mM in DMSO	￥800.00 T28940-1ml ￥800.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T28940-1ml

10mM in DMSO

￥800.00

货期：3-5天

产品描述：

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

靶点：

MIC: 0.3 µM (MSSA), 0.3-1 µM (MRSA), 0.3 µM (VISA)

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. 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.T1/2=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.

参考文献：

1. Le P, et al. Repurposing human kinase inhibitors to create an antibiotic active against drug-resistant Staphylococcus aureus, persisters and biofilms. Nat Chem. 2019 Dec 16.

溶解性：

Soluble in DMSO

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.534 ml	12.668 ml	25.337 ml
5 mM	0.507 ml	2.534 ml	5.067 ml
10 mM	0.253 ml	1.267 ml	2.534 ml
50 mM	0.051 ml	0.253 ml	0.507 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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