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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s36沙龙会进行
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s36沙龙会进行
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s36沙龙会进行
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s36沙龙会进行
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s36沙龙会合成了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s36沙龙会合成了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s36沙龙会进行
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s36沙龙会进行
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s36沙龙会进行
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s36沙龙会进行
Jul 05,2023
合成具有体内抗肿瘤活性的强效PD-L1抑制剂，并进行生物学评价和机制研究。PK研究通过s36沙龙会进行
PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified compound L7 as a potent PD-L1 inhibitor that blocked PD-1/PD-L1 interaction. Pharmacokinetic (PK) studies demonstrated that L7 was orally bioavailable. PK studies were conducted by Medicilon.
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合成具有体内抗肿瘤活性的强效PD-L1抑制剂，并进行生物学评价和机制研究。PK研究通过s36沙龙会进行
Jul 05,2023
SLL-1206是一种κ阿片受体激动剂，具有显著改善的理化和药代动力学特性。作者感谢s36沙龙会对SLL-1206进行的药代动力学研究
The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects. The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.
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SLL-1206是一种κ阿片受体激动剂，具有显著改善的理化和药代动力学特性。作者感谢s36沙龙会对SLL-1206进行的药代动力学研究
Jul 05,2023
苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中，所有肝微粒体测定均通过s36沙龙会进行
Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. XY123 potently inhibits the RORγ transcription activity with an IC50 value of 64 nM. XY123 demonstrates good metabolic stability and a pharmacokinetics property with reasonable oral bioavailability (32.41%) and moderate half-life (4.98 h). All liver microsome assays were performed by Medicilon.
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苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中，所有肝微粒体测定均通过s36沙龙会进行
Jul 05,2023
zapERtrap：光调节的内质网释放系统揭示了意想不到的神经元运输途径，Zapalog的合成通过s36沙龙会进行
zapERtrap opens the door to previously unapproachable questions concerning how proteins are processed, trafficked, and secreted in space and time in complex cellular environments. zapERtrap relies on a small-molecule protein dimerizer zapalog, which consists of the antibiotic trimethoprim tethered to a synthetic ligand of FK506-binding protein through a photocleavable linker. Synthesis of zapalog was performed by Medicilon.
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zapERtrap：光调节的内质网释放系统揭示了意想不到的神经元运输途径，Zapalog的合成通过s36沙龙会进行
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