南宫NG28

YY201获得临床获批不仅代表了宇耀生物又一沉要突破
，验证了宇耀生物超等分子胶技术平台和AI药物辅助开发平台的创新能力
，同时也证了然南宫NG28临床前钻研的技术服务力量。

南宫NG28为NB002提供了安全性评价、药代动力学等临床前钻研服务
，助力其IND申请顺利获FDA临床许可。

南宫NG28为BIOT-001的研发提供了从靶点到IND申报的临床前研发服务
，全力促成该项目高质高效实现。

?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.

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.

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.

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.

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.

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.

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.