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临床前CDMO研发化合物筛选
Lesinurad
中文名称:雷西纳德
CAS号:878672-00-5
分子式: C17H14BrN3O2S 分子量: 404.28
产品形式: free base
研发状态: Completed
研发用途: Gout
研究机构: Ardea Biosciences Inc.
研发日期: Oct-09
研发阶段: Phase 2
Lesinurad (RDEA-594) is a selective uric acid reabsorption inhibitor (SURI) under investigation for treatment of gout in combination with xanthine oxidase inhibitors. Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
D-Tagatose
中文名称:D-塔格糖
CAS号:87-81-0
分子式: C6H12O6 分子量: 180.16
产品形式: free base
研发状态: Completed
研发用途: Type 2 Diabetes
研究机构: Robert Lodder; University of Kentucky; Spherix Incorporated
研发日期: Feb-08
研发阶段: Phase 2
D-Tagatose is an isomer of fructose and is used as a sweetener in beverages, yogurt, creams, and dietetic candy.
Crizotinib (PF-02341066)
中文名称:克唑替尼
CAS号:877399-52-5
分子式: C21H22Cl2FN5O 分子量: 450.34
产品形式: free base
研发状态: Not yet recruiting
研发用途: Non-Small Cell Lung Cancer
研究机构: Han Xu M.D. Ph.D. FAPCR Sponsor-Investigator IRB Chair; Medicine Invention Design Inc
研发日期: March 28 2024
研发阶段: Phase 2 : Phase 3
Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Anacetrapib (MK-0859)
中文名称:安塞曲匹
CAS号:875446-37-0
分子式: C30H25F10NO3 分子量: 637.51
产品形式: free base
研发状态: Completed
研发用途: Dyslipidemia
研究机构: Merck Sharp & Dohme LLC
研发日期: Jun-10
研发阶段: Phase 1
Anacetrapib (MK0859) is a potent, selective, reversible rhCETP and mutant CETP(C13S) inhibitor with IC50 of 7.9 nM and 11.8 nM, increases HDL-C and decreases LDL-C, does not increase aldosterone or blood pressure. Phase 3.
Quisinostat (JNJ-26481585) 2HCl
CAS号:875320-31-3
分子式: C21H28Cl2N6O2 分子量: 467.39
产品形式: Dihydrochloride
研发状态: Completed
研发用途: Ovarian Cancer
研究机构: NewVac LLC; Janssen Pharmaceutica N.V. Belgium
研发日期: Sep-15
研发阶段: Phase 2
Quisinostat (JNJ-26481585) 2HCl is a novel second-generation HDAC inhibitor with highest potency for HDAC1 with IC50 of 0.11 nM in a cell-free assay, modest potent to HDACs 2, 4, 10, and 11; greater than 30-fold selectivity against HDACs 3, 5, 8, and 9 and lowest potency to HDACs 6 and 7. Phase 2.
Fidaxomicin
中文名称:非达霉素
CAS号:873857-62-6
分子式: C52H74Cl2O18 分子量: 1058.04
产品形式: free base
研发状态: Recruiting
研发用途: Clostridium Difficile Infection
研究机构: McGill University Health Centre/Research Institute of the McGill University Health Centre; Canadian Institutes of Health Research (CIHR)
研发日期: November 19 2020
研发阶段: Phase 3
Fidaxomicin (OPT-80, PAR-101,Dificid) is a narrow spectrum macrocyclic antibiotic that inhibits RNA polymerase sigma subunit.
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