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Jul 06,2023
表观遗传修饰，如DNA甲基化，在遗传信息的表达中发挥着重要作用。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 µM. 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发挥着重要作用。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前景的靶点。化合物W8对FBPase表现出高选择性。W8的药代动力学研究通过AG真人国际(中国)官方官网进行
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前景的靶点。化合物W8对FBPase表现出高选择性。W8的药代动力学研究通过AG真人国际(中国)官方官网进行
Jul 06,2023
药物发现中的挑战之一是识别高质量的先导化合物。此研究中PK结果表明L12可作为针对PDE5的先导化合物，进一步研究和开发。L12的PK分析通过AG真人国际(中国)官方官网进行
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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药物发现中的挑战之一是识别高质量的先导化合物。此研究中PK结果表明L12可作为针对PDE5的先导化合物，进一步研究和开发。L12的PK分析通过AG真人国际(中国)官方官网进行
Jul 06,2023
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AG真人国际(中国)官方官网进行
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AG真人国际(中国)官方官网进行
Jul 06,2023
XY153是一种有潜力的先导化合物，可用于开发针对急性髓系白血病。XY153在体外具有良好的代谢稳定性。所有肝微粒体测定均通过AG真人国际(中国)官方官网进行
Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The representative Compound 8l (XY153), a novel BD2-selective BET inhibitor, potently binds to BRD4 BD2 with an IC50 value of 0.79 nM. XY153 displayed potent antiproliferative activity against multiple tumor cell lines. XY153 also demonstrated good metabolic stability in vitro. These data indicate that XY153 may serve as a new and valuable lead compound for the development of potential therapeutics against acute myeloid leukemia (AML). All liver microsome assays were performed by Medicilon.
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XY153是一种有潜力的先导化合物，可用于开发针对急性髓系白血病。XY153在体外具有良好的代谢稳定性。所有肝微粒体测定均通过AG真人国际(中国)官方官网进行
Jul 06,2023
Y180是一种口服Mpro抑制剂，可有效对抗野生型SARS-CoV-2及其变种。Y180在小鼠、大鼠和狗中具有良好的PK特性
Y180, an orally available Mpro inhibitor, is effective against wild-type SARS-CoV-2 and variants. Y180 displayed satisfying PK properties in mice, rats and dogs, with oral bioavailabilities of 92.9%, 31.9% and 85.7%, respectively. The in vivo PK properties of Y180 were evalsuated. All procedures related to animal handling, care and treatment in PK studies were performed according to approved guidelines. The PK studies were approved by the Ethics Committee of Medicilon.
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Y180是一种口服Mpro抑制剂，可有效对抗野生型SARS-CoV-2及其变种。Y180在小鼠、大鼠和狗中具有良好的PK特性
Jul 06,2023
Ulotaront是一种具有5-HT1A激动剂活性的TAAR1 激动剂，可用于治疗精神分裂症。Ulotaront在大鼠脑中的分布和在猴血浆中的PK研究通过AG真人国际(中国)官方官网进行
Ulotaront (SEP-363856) is a TAAR1 agonist with 5-HT1A agonist activity currently in clinical development for the treatment of Schizophrenia. Ulotaront exhibits rapid absorption, greater than 70% bioavailability, and good penetration across the blood–brain barrier in preclinical species. The distribution of Ulotaront to rat brain was conducted at Medicilon/MPI Preclinical Research. Ulotaront monkey plasma PK was conducted at Medicilon/MPI Preclinical Research.
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Ulotaront是一种具有5-HT1A激动剂活性的TAAR1 激动剂，可用于治疗精神分裂症。Ulotaront在大鼠脑中的分布和在猴血浆中的PK研究通过AG真人国际(中国)官方官网进行
Jul 06,2023
基于构效关系分析，合成了一种结构简化但具有优异防污活性的化合物。优化后的化合物通过AG真人国际(中国)官方官网合成
Biofouling poses one of the most serious problems to marine industry and aquaculture development. Five structurally similar compounds were isolated from the crude extract of a marine Streptomyces strain. Antifouling activities of these compounds and four other structurally-related compounds isolated from another marine Streptomyces species were compared to generate structure–activity relationship data. Based on structure–activity relationship analysis, another compound with a simplified structure but excellent antifouling activities was synthesized. The optimized compound was synthesized by Medicilon.
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基于构效关系分析，合成了一种结构简化但具有优异防污活性的化合物。优化后的化合物通过AG真人国际(中国)官方官网合成
Jul 06,2023
开发和验证大鼠血浆中Nobiliside A定量的LC/MS/MS方法
Nobiliside A, a new triterpene glycoside, exhibits some biological activities including antifungal and cytotoxic effects. A LC/MS/MS method was developed and validated for determination of Nobiliside A in rat plasma, would prove to be useful for other pharmacokinetic assessments. Male SD rats were housed in Medicilon animal facility. The animal experiments of the present study were approved by IACUC of Medicilon and were carried out in accordance with the SOPs of the facility.
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开发和验证大鼠血浆中Nobiliside A定量的LC/MS/MS方法
Jul 06,2023
4-正丁基间苯二酚是一种高效的酪氨酸酶抑制剂，可用于化妆品中以达到脱色的目的。其中经皮吸收和皮肤分布研究通过AG真人国际(中国)官方官网进行
4-n-butyl resorcinol (4-nBR) is a highly effective tyrosinase inhibitor, and can be used in cosmetic product for depigmentation purpose. Its efficacy correlates with 4-nBR that absorbed by skin. In this study, skin distribution of 4-nBR within either human or pig skin ex vivo was studied and compared by three independent laboratories. Good agreement was observed in each compartment considering usual inter-lab variability. The percutaneous absorption and skin distribution studies were carried out by L'Oréal (lab A), Fudan University (lab B), and Medicilon (lab C).
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4-正丁基间苯二酚是一种高效的酪氨酸酶抑制剂，可用于化妆品中以达到脱色的目的。其中经皮吸收和皮肤分布研究通过AG真人国际(中国)官方官网进行