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    中國：

    Email: marketing@yakkaa.com

    業務谘詢專線：400-780-8018

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Jul 06,2023
研究人員成功發現了一種口服PROTAC降解劑SIAIS164018，具有良好的體內耐受性。PK和MTD研究通過hjc黄金城進行
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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研究人員成功發現了一種口服PROTAC降解劑SIAIS164018，具有良好的體內耐受性。PK和MTD研究通過hjc黄金城進行
Jul 06,2023
開發具有口服活性的高度選擇性卵泡刺激激素受體激動劑，且進行臨床前研究。其中對大鼠和狗的毒理學評估通過hjc黄金城進行
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 evaluated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evaluations 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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開發具有口服活性的高度選擇性卵泡刺激激素受體激動劑，且進行臨床前研究。其中對大鼠和狗的毒理學評估通過hjc黄金城進行
Jul 06,2023
PARP1/2抑製劑有治療腫瘤的潛力，PARP1/2抑製實驗通過hjc黄金城進行
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抑製劑有治療腫瘤的潛力，PARP1/2抑製實驗通過hjc黄金城進行
Jul 06,2023
使用hjc黄金城硒代氨基酸培養基產品發表的學術文獻
hjc黄金城提供全套M9硒代蛋氨酸（SeMET）培養基，可用於IPTG誘導的大腸杆菌表達係統，生產硒代蛋氨酸標記的蛋白，運用多波長反常散射（MAD）方法進行蛋白質晶體學研究。
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使用hjc黄金城硒代氨基酸培養基產品發表的學術文獻
Jul 05,2023
設計合成一種高度選擇性的H435R突變敏感的甲狀腺激素受體β激動劑，PK分析通過hjc黄金城進行
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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設計合成一種高度選擇性的H435R突變敏感的甲狀腺激素受體β激動劑，PK分析通過hjc黄金城進行
Jul 05,2023
研究人員設計合成STAT3和HDAC雙通路抑製劑用於治療實體腫瘤，PK實驗通過hjc黄金城進行
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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研究人員設計合成STAT3和HDAC雙通路抑製劑用於治療實體腫瘤，PK實驗通過hjc黄金城進行
Jul 05,2023
阿帕替尼通過VEGFR2通路抑製紫杉醇對胃癌細胞的耐藥性
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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阿帕替尼通過VEGFR2通路抑製紫杉醇對胃癌細胞的耐藥性
Jul 05,2023
研究人員報告了一種具有細胞滲透性的選擇性METTL3納摩爾抑製劑UZH1a，作者感謝hjc黄金城合成了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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研究人員報告了一種具有細胞滲透性的選擇性METTL3納摩爾抑製劑UZH1a，作者感謝hjc黄金城合成了UZH1a和UZH1b
Jul 05,2023
研究人員設計並合成了一種光籠PI3K抑製劑1，它可以通過紫外線照射激活，釋放出高效PI3K抑製劑2。化合物1和2的ADME研究通過hjc黄金城進行
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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研究人員設計並合成了一種光籠PI3K抑製劑1，它可以通過紫外線照射激活，釋放出高效PI3K抑製劑2。化合物1和2的ADME研究通過hjc黄金城進行
Jul 05,2023
RIPK2激酶參與多種慢性炎症，UH15-15抑製RIPK2激酶並具有良好的體外ADME和PK特性，PK研究通過hjc黄金城進行
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激酶參與多種慢性炎症，UH15-15抑製RIPK2激酶並具有良好的體外ADME和PK特性，PK研究通過hjc黄金城進行