|
EN
|
EN
EN
  • 业务咨询

    中国:

    Email: marketing@medicilon.com.cn

    业务咨询专线:400-780-8018

    (仅限服务咨询,其他事宜请拨打川沙总部电话)

    川沙总部电话: +86 (21) 5859-1500

    海外:

    +1(626)986-9880(U.S. - West Coast)

    0044 7790 816 954 (Europe)

    Email:marketing@medicilon.com

在线留言×
点击切换
Customer Center
客户中心

ANO1是一个潜在的镇痛靶点。DFBTA是一种有效的ANO1抑制剂,具有优异的药代动力学特性。体内PK测试通过美迪西进行

2023-07-06
|
访问量:

Current pain management is largely limited to opioids and non-steroidal anti-inflammatory drugs. Developing new analgesic drugs remains important to address the unmet medical needs of chronic pain patients. Calcium-activated chloride channel anoctamin-1 (ANO1) is a potential analgesic target. DFBTA is a potent inhibitor with the IC50 of 24 nM. DFBTA shows very weak cytotoxicity, cardiotoxicity, and acute toxicity, as well as excellent pharmacokinetics properties with oral bioavailability >75% and little brain penetration (<1.5% brain/plasma). In vivo PK were tested by Medicilon

32.jpg

Reference:

Yuxi Wang, et al. Optimization of 4-arylthiophene-3-carboxylic acid derivatives as inhibitors of ANO1: Lead optimization studies toward their analgesic efficacy for inflammatory pain. Eur J Med Chem. 2022 Jul 5;237:114413. doi: 10.1016/j.ejmech.2022.114413. 

相关新闻
×
搜索验证
点击切换