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Jul 06,2023
PARP1/2抑制剂有治疗肿瘤的潜力，PARP1/2抑制实验通过合乐HL8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抑制实验通过合乐HL8进行
Jul 06,2023
使用合乐HL8硒代氨基酸培养基产品发表的学术文献
合乐HL8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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使用合乐HL8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分析通过合乐HL8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分析通过合乐HL8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实验通过合乐HL8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实验通过合乐HL8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，作者感谢合乐HL8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 s 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，作者感谢合乐HL8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研究通过合乐HL8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研究通过合乐HL8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研究通过合乐HL8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研究通过合乐HL8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研究通过合乐HL8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研究通过合乐HL8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。作者感谢合乐HL8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 s 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。作者感谢合乐HL8对SLL-1206进行的药代动力学研究