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临床前CDMO研发化合物筛选
Berberine chloride (NSC 646666)
中文名称:盐酸黄连素; 盐酸小檗碱
CAS号:633-65-8
分子式: C20H18NO4.Cl 分子量: 371.81
产品形式: chloride
研发状态: Not yet recruiting
研发用途: Pharmacokinetic Study in Healthy Volunteers
研究机构: University Medicine Greifswald
研发日期: March 4 2024
研发阶段: Not Applicable
Berberine chloride (NSC 646666, Natural Yellow 18) is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.
Hydroxyprogesterone caproate
中文名称:己酸孕酮
CAS号:630-56-8
分子式: C27H40O4 分子量: 428.60
产品形式: free base
研发状态: Completed
研发用途: Pregnancy
研究机构: Lumara Health Inc.
研发日期: Jul-13
研发阶段: Phase 1
Hydroxyprogesterone Caproate (17α-Hydroxyprogesterone hexanoate, 17α-Hydroxyprogesterone caproate) is a synthetic progestational agent. It binds to and activates nuclear progesterone receptors in the reproductive system and inhibits ovulation and an alteration in the cervical mucus and endometrium.
Asunaprevir (BMS-650032)
中文名称:阿那匹韦
CAS号:630420-16-5
分子式: C35H46ClN5O9S 分子量: 748.29
产品形式: free base
研发状态: Withdrawn
研发用途: Hepatitis C
研究机构: Bristol-Myers Squibb
研发日期: November 30 2018
研发阶段: --
Asunaprevir (BMS-650032) is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
Staurosporine (AM-2282)
中文名称:星孢菌素
CAS号:62996-74-1
分子式: C28H26N4O3 分子量: 466.53
产品形式: Free Base
研发状态: Withdrawn
研发用途: Ankle Fractures; Post-traumatic Osteoarthritis; Osteoarthritis Ankle
研究机构: University of Iowa
研发日期: Dec-24
研发阶段: Not Applicable
Staurosporine (AM-2282, Antibiotic AM-2282, STS) is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of 2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc. Phase 3.
SU14813
CAS号:627908-92-3
分子式: C23H27FN4O4 分子量: 442.48
产品形式: Free base
研发状态: Completed
研发用途: Breast Neoplasms
研究机构: Pfizer
研发日期: Apr-06
研发阶段: Phase 2
SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity.
Captopril
中文名称:卡托普利
CAS号:62571-86-2
分子式: C9H15NO3S 分子量: 217.29
产品形式: free base
研发状态: Withdrawn
研发用途: Healthy Volunteers
研究机构: GlaxoSmithKline
研发日期: April 21 2022
研发阶段: Phase 1
Captopril (SQ 14225,Capoten) is an angiotensin-converting enzyme (ACE) inhibitor with IC50 of 6 nM.
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