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Aug 21,2023
TAK-931是一种高效的CDC7抑制剂，通过抑制CDC7来抑制DNA复制，具有抗肿瘤功效，体内药效研究通过william威廉亚洲官方举行
Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell division cycle 7 (CDC7) has attracted attention as a target. Researchers have developed an oral CDC7-selective inhibitor, TAK-931, as a candidate clinical anticancer drug. TAK-931 demonstrated marked, dose-dependent antitumor activity, without severe body weight loss. Antitumor efficacy studies for TAK-931 were carried out in two pancreatic PDX models, PHTX-249Pa and PHTXM-97Pa, at Medicilon.
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TAK-931是一种高效的CDC7抑制剂，通过抑制CDC7来抑制DNA复制，具有抗肿瘤功效，体内药效研究通过william威廉亚洲官方举行
Jul 17,2023
AP39是一种新合成的线粒体靶向的H2S供体，本研究中AP39通过william威廉亚洲官方设计和合成
?Alzheimer's disease (AD) is the most universal age-related neurodegenerative disease. AP39 is a newly synthesized mitochondrially targeted H2S donor on mitochondrial function. AP39 increases intracellular H2S levels, mainly in mitochondrial regions. AP39 exerts dose-dependent effects on mitochondrial activity in APP/PS1 neurons. AP39, a novel mitochondria-targeted H2S donor, was designed and synthesized by Medicilon.
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AP39是一种新合成的线粒体靶向的H2S供体，本研究中AP39通过william威廉亚洲官方设计和合成
Jul 06,2023
发明新型RAGE/SERT双重抑制剂，可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托william威廉亚洲官方举行
Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of β-amyloid (Aβ) peptide plaques, neurofibrillary tangles, and neuroinflammation. Receptor for advanced glycation end products (RAGE) belongs to the immunoglobulin superfamily, which functions as a cell surface acceptor for Aβ peptide. RAGE plays an important role in the Aβ-mediated neuronal damage that closely related to the pathogenesis of AD. In this study, Compound 12 showed good dual-target bioactivities against RAGE and SERT in vitro, good liver microsomal stability, and acceptable pharmacokinetic properties. Pharmacokinetic studies were commissioned by Medicilon.
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发明新型RAGE/SERT双重抑制剂，可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托william威廉亚洲官方举行
Jul 06,2023
TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂，具有优异的Caco-2渗透性。Caco-2 渗透性测定通过william威廉亚洲官方举行
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers”and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.
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TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂，具有优异的Caco-2渗透性。Caco-2 渗透性测定通过william威廉亚洲官方举行
Jul 06,2023
IAP卵白是有吸引力的癌症治疗靶点。SM-406 是一种口服有用的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过william威廉亚洲官方举行
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators. IAP proteins are attractive cancer therapeutic targets. SM-406 (compound 2) is a potent and orally bioavailable antagonist of the IAPs. Pharmacokinetic (PK) studies of SM-406 (compound 2) in male Sprague Dawley rats, beagle dogs and cynomolgus monkeys (non-human primates) were performed by the Division of Pharmacokinetics and Metabolism, Medicilon. SM-406 (compound 2) has an excellent PK profile and good oral bioavailability in each of these four species.
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IAP卵白是有吸引力的癌症治疗靶点。SM-406 是一种口服有用的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过william威廉亚洲官方举行
Jul 06,2023
设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂，并举行生物学评价。其中药代动力学剖析通过william威廉亚洲官方举行
Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric cancer. The pharmacokinetical profile (PK) of 8f was tested in SD rats. Compound 8f showed an acceptable half-time of 3 h and displayed moderate maximum concentrations, which is enough to meet the concentration of the compound 8f to exert its efficacy in vivo. The pharmacokinetic analysis was performed by the testing service provided by Medicilon.
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设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂，并举行生物学评价。其中药代动力学剖析通过william威廉亚洲官方举行
Jul 06,2023
表观遗传修饰，如DNA甲基化，在遗传信息的表达中施展着主要作用。DNA甲基转移酶维持DNA甲基化，是肿瘤化疗的一个有吸引力的靶点
Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC50 value of 5.0??M. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.
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表观遗传修饰，如DNA甲基化，在遗传信息的表达中施展着主要作用。DNA甲基转移酶维持DNA甲基化，是肿瘤化疗的一个有吸引力的靶点
Jul 06,2023
FBPase是与肿瘤和2型糖尿病相关的一个有远景的靶点�；衔颳8对FBPase体现出高选择性。W8的药代动力学研究通过william威廉亚洲官方举行
Fructose-1,6-bisphosphatase (FBPase) is a promising target associated with cancer and type 2 diabetes. Compounds W8 and W8k exhibit high selectivity against FBPase and W8 effectively reduces blood glucose in an Institute of Cancer Research (ICR) mice model and dose-dependent inhibition of glucose production in a primary mouse hepatocyte model. The pharmacokinetic studies of W8 and its leaving group saccharin were performed by Medicilon.
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FBPase是与肿瘤和2型糖尿病相关的一个有远景的靶点�；衔颳8对FBPase体现出高选择性。W8的药代动力学研究通过william威廉亚洲官方举行
Jul 06,2023
药物发明中的挑战之一是识别高质量的先导化合物。此研究中PK效果批注L12可作为针对PDE5的先导化合物，进一步研究和开发。L12的PK剖析通过william威廉亚洲官方举行
Scaffold hopping refers to computer-aided screening for active compounds with different structures against the same receptor to enrich privileged scaffolds, which is a topic of high interest in organic and medicinal chemistry. One of the biggest challenges in drug discovery is to identify high-quality hit and lead compounds. Lead L12 had an IC50 of 8.7 nM and exhibited a different binding pattern in its crystal structure with PDE5 from the famous starting drug tadalafil, and PK results indicate that L12 could be used as a promising lead for further development. Pharmacokinetic properties of L12 were analyzed by Medicilon.
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药物发明中的挑战之一是识别高质量的先导化合物。此研究中PK效果批注L12可作为针对PDE5的先导化合物，进一步研究和开发。L12的PK剖析通过william威廉亚洲官方举行
Jul 06,2023
ANO1是一个潜在的镇痛靶点。DFBTA是一种有用的ANO1抑制剂，具有优异的药代动力学特征。体内PK测试通过william威廉亚洲官方举行
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.
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ANO1是一个潜在的镇痛靶点。DFBTA是一种有用的ANO1抑制剂，具有优异的药代动力学特征。体内PK测试通过william威廉亚洲官方举行
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