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Jul 06,2023
研究人员成功发现了一种口服PROTAC降解剂SIAIS164018，具有良好的体内耐受性。PK和MTD研究通过AG真人国际(中国)官方官网进行
PROTAC is an attractive technology in drug discovery. Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 which degrades not only ALK or mutant EGFR but also oncoproteins involved in metastasis. SIAIS164018 is orally bioavailable and well tolerated in vivo. Pharmacokinetic and maximal tolerated dose (MTD) assays were performed by Medicilon.
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研究人员成功发现了一种口服PROTAC降解剂SIAIS164018，具有良好的体内耐受性。PK和MTD研究通过AG真人国际(中国)官方官网进行
Jul 06,2023
开发具有口服活性的高度选择性卵泡刺激激素受体激动剂，且进行临床前研究。其中对大鼠和狗的毒理学评估通过AG真人国际(中国)官方官网进行
TOP5300 is an orally active follicle stimulating hormone receptor allosteric agonist that provides a preferred treatment for over 16 million infertile women of reproductive age in low complexity methods or in high complexity methods. TOP5300 was evalsuated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evalsuations were performed in both rat and dog as the second species according to the guidance from FDA. These assays were performed by Medicilon.
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开发具有口服活性的高度选择性卵泡刺激激素受体激动剂，且进行临床前研究。其中对大鼠和狗的毒理学评估通过AG真人国际(中国)官方官网进行
Jul 06,2023
PARP1/2抑制剂有治疗肿瘤的潜力，PARP1/2抑制实验通过AG真人国际(中国)官方官网进行
Poly ADP-ribose polymerases (PARPs) are a family of enzymes related to DNA damage repair process. Inhibition of PARP1/2 accelerates the damage of injured DNA, which is synthetically lethal to DNA-repairing-deficient cancer cells, such as BRCA1/2-deficient cells. PARP1/2 inhibitors could be a promising candidate for the treatment of cancer. The PARP1 and PARP2 inhibition assays were performed by Medicilon.
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PARP1/2抑制剂有治疗肿瘤的潜力，PARP1/2抑制实验通过AG真人国际(中国)官方官网进行
Jul 06,2023
使用AG真人国际(中国)官方官网硒代氨基酸培养基产品发表的学术文献
AG真人国际(中国)官方官网提供全套M9硒代蛋氨酸（SeMET）培养基，可用于IPTG诱导的大肠杆菌表达系统，生产硒代蛋氨酸标记的蛋白，运用多波长反常散射（MAD）方法进行蛋白质晶体学研究。
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使用AG真人国际(中国)官方官网硒代氨基酸培养基产品发表的学术文献
Jul 05,2023
设计合成一种高度选择性的H435R突变敏感的甲状腺激素受体β激动剂，PK分析通过AG真人国际(中国)官方官网进行
Thyroid hormone receptors (TRs) are ligand-dependent transcription factors that belong to the nuclear receptor superfamily and also participate in important physiological functions. In this study, Compound 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH). Compound 16g showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. PK properties of Compound 16g were analyzed by Medicilon.
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设计合成一种高度选择性的H435R突变敏感的甲状腺激素受体β激动剂，PK分析通过AG真人国际(中国)官方官网进行
Jul 05,2023
研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤，PK实验通过AG真人国际(中国)官方官网进行
The inhibition of HDACs will lead to compensated activation of a notorious cancer-related drug target, STAT3, in breast cancer through a cascade, which probably limits the anti-proliferation effect of HDAC inhibitors in solid tumors. Herein, researchers synthesized a series of potent pterostilbene hydroxamic acid derivatives with dual-target inhibition activity. The pharmacokinetic experiment in SD Rats was carried out by Medicilon.
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研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤，PK实验通过AG真人国际(中国)官方官网进行
Jul 05,2023
阿帕替尼通过VEGFR2通路抑制紫杉醇对胃癌细胞的耐药性
Overexpression of VEGFR2 can offset the rescue effect of Apatinib on Paclitaxel-induced drug resistance of MGC803 cells. Apatinib inhibits Paclitaxel resistance of MGC803 cells via the VEGFR2 signaling pathway. In this research, the VEGFR2 sequences were designed and then amplified by RT-PCR. The sequences were then ligated with a pcDNA3.0 plasmid to construct a recombinant pcDNA3.0-VEGFR2 vector (Medicilon).
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阿帕替尼通过VEGFR2通路抑制紫杉醇对胃癌细胞的耐药性
Jul 05,2023
研究人员报告了一种具有细胞渗透性的选择性METTL3纳摩尔抑制剂UZH1a，作者感谢AG真人国际(中国)官方官网合成了UZH1a和UZH1b
The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification of RNA. Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable, while its enantiomer UZH1b is essentially inactive. The authors thank Medicilon for the synthesis of the UZH1a and UZH1b compounds.
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研究人员报告了一种具有细胞渗透性的选择性METTL3纳摩尔抑制剂UZH1a，作者感谢AG真人国际(中国)官方官网合成了UZH1a和UZH1b
Jul 05,2023
研究人员设计并合成了一种光笼PI3K抑制剂1，它可以通过紫外线照射激活，释放出高效PI3K抑制剂2。化合物1和2的ADME研究通过AG真人国际(中国)官方官网进行
Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades. In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies of compounds 1 and 2 were conducted by Medicilon. Medicilon's pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody.
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研究人员设计并合成了一种光笼PI3K抑制剂1，它可以通过紫外线照射激活，释放出高效PI3K抑制剂2。化合物1和2的ADME研究通过AG真人国际(中国)官方官网进行
Jul 05,2023
RIPK2激酶参与多种慢性炎症，UH15-15抑制RIPK2激酶并具有良好的体外ADME和PK特性，PK研究通过AG真人国际(中国)官方官网进行
Receptor interacting protein kinase-2 (RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase (IC50=8 nM) and demonstrates favorable in vitro ADME and pharmacokinetic properties. The pharmacokinetic study was conducted by Medicilon.
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RIPK2激酶参与多种慢性炎症，UH15-15抑制RIPK2激酶并具有良好的体外ADME和PK特性，PK研究通过AG真人国际(中国)官方官网进行