3-肼基喹喔啉-2(1H)-硫酮
- CAS号:13080-21-2
- 英文名:3-HYDRAZINO-QUINOXALINE-2-THIOL
- 中文名:3-肼基喹喔啉-2(1H)-硫酮
- CBNumber:CB1135666
- 分子式:C8H8N4S
- 分子量:192.24
- MOL File:13080-21-2.mol
- 熔点 :254 °C (decomp)(Solv: ethanol (64-17-5))
- 沸点 :376.1±25.0 °C(Predicted)
- 密度 :1.55±0.1 g/cm3(Predicted)
- 酸度系数(pKa) :7.91±0.20(Predicted)
- 形态 :Solid
- 颜色 :Light yellow to yellow
3-肼基喹喔啉-2(1H)-硫酮性质、用途与生产工艺
- 生物活性 HPi1 是一种针对幽门螺杆菌 (Helicobacter pylori) 的有效，选择性和具有口服活性的抗菌剂，IC50 为 0.24 μM，MIC 为 0.08-0.16 μg/mL。HPi1 对其他细菌无活性，包括肠道菌干酪乳杆菌，罗伊氏乳杆菌和长双歧杆菌。
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靶点
IC50: 0.24 μM ( Helicobacter pylori )
MIC: 0.08-0.16 μg/mL ( Helicobacter pylori ) -
体外研究
The MIC against H. pylori isolates ranged from 0.002-0.032 μg/mL (0.01-0.17 μM) in the agar dilution assay. HPi1 is effective against the clarithromycin-resistant strains ARHp172 (MIC of 0.004–0.016 μg/mL) and ARHp246 (MIC of 0.008–0.032 μg/mL).
HPi1 has some activity against the Bacteroides species , but at concentrations at least 18-fold higher than the H. pylori MIC. More potent activity is detected for Campylobacter jejuni with an MIC of 0.3 μg/mL.
HPi1 has good physicochemical and pharmacological properties, including determining the aqueous solubility (19 μg/mL), human plasma protein binding (93% bound), stability with human liver microsomes (T 1/2 of 1.3 hours) and the ability to passively permeate membranes. -
体内研究
HPi1 (6.25-50 mg/kg; Oral gavage; once a day; for 3 days; female C57BL/6 mice) treatment decreases colony counts below the limit of detection at doses of 25 or 50 mg/kg/day.
Animal Model: Adult specific-pathogen-free female C57BL/6 mice (6-8-week-old) fed with H. pylori SS1 suspension Dosage: 6.25 mg/kg, 12.5 mg/kg, 25 mg/kg, 50 mg/kg Administration: Oral gavage; once a day; for 3 days Result: Reduced colony counts to below the limit of detection.
- 公司名称：Fluorochem Ltd
- 联系电话：--
- 电子邮件：vernam@fluorochem.co.uk
- 国家：英国
- 产品数：6375
- 优势度：65
- 公司名称：FLRO-SR
- 联系电话：--
- 电子邮件：enquiries@fluorochem.co.uk
- 国家：英国
- 产品数：6401
- 优势度：74
