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    中國：

    Email: marketing@yakkaa.com

    業務谘詢專線：400-780-8018

    （僅限服務谘詢，其他事宜請撥打川沙總部電話）

    川沙總部電話: +86 (21) 5859-1500

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    0044 7790 816 954 (Europe)

    Email:marketing@medicilon.com

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Jul 05,2023
合成一類新型選擇性TNIK抑製劑並評估其抗結直腸癌作用，PK研究通過hjc黄金城進行
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of 21k was carried out through services provided by Medicilon.
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合成一類新型選擇性TNIK抑製劑並評估其抗結直腸癌作用，PK研究通過hjc黄金城進行
Jul 05,2023
用於治療非酒精性脂肪性肝炎的PPARα/δ 雙重激動劑的設計合成和生物學評價，PK研究、hERG研究和Ames試驗通過hjc黄金城進行
Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.
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用於治療非酒精性脂肪性肝炎的PPARα/δ 雙重激動劑的設計合成和生物學評價，PK研究、hERG研究和Ames試驗通過hjc黄金城進行
Jul 05,2023
ARD-2585是一種口服有效的PROTAC雄激素受體降解劑，可用於治療晚期前列腺癌。肝微粒體穩定性測定、血漿穩定性測定和hERG測定通過hjc黄金城進行
A PROTAC-based androgen receptor (AR) degrader is a bifunctional small molecule, consisting of an AR ligand that binds to AR protein, and a ligand that binds to and recruits an E3 ligase complex, tethered together through a linker. Researchers report the discovery of exceptionally potent and orally bioavailable PROTAC AR degrader ARD-2585 (Compound 43). ARD-2585 is a promising AR degrader for extensive investigations for the treatment of advanced prostate cancer. The liver microsomal stability assay was performed by Medicilon. The plasma stability assay was performed by Medicilon. The hERG assay was performed by Medicilon.
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ARD-2585是一種口服有效的PROTAC雄激素受體降解劑，可用於治療晚期前列腺癌。肝微粒體穩定性測定、血漿穩定性測定和hERG測定通過hjc黄金城進行
Jul 05,2023
選擇性小分子c-Myc降解劑可有效消退c-Myc過表達的腫瘤，表麵等離子共振 (SPR) 實驗通過hjc黄金城進行
Cancer is one of the leading causes of death worldwide. MYC oncogene is involved in the majority of human cancers and is often associated with poor outcomes. WBC100, a novel oral active molecule glue that selectively degrades c-Myc protein over other proteins and potently kills c-Myc overexpressing cancer cells is reported. Researchers performed direct binding assay of WBC100 with c-Myc on biosensor chip by surface plasmon resonance (SPR). SPR experiments were performed using a Biacore T200 instrument by Medicilon.
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選擇性小分子c-Myc降解劑可有效消退c-Myc過表達的腫瘤，表麵等離子共振 (SPR) 實驗通過hjc黄金城進行
Jun 28,2023
SAHA可有效恢複阿爾茨海默病模型的記憶能力，本研究中SAHA通過hjc黄金城合成
SAHA was synthesized by Medicilon and was given to mice as 50 mg/kg doses. Injections (10 mL/kg) were given intraperitoneally and were alternated daily between left and right sides of the abdomen. Chronic treatments of SAHA completely restored performance deficits in APP/PS1 mice.
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SAHA可有效恢複阿爾茨海默病模型的記憶能力，本研究中SAHA通過hjc黄金城合成
Jun 28,2023
TAK-243是一種有效的泛素激活酶小分子抑製劑，具有體內抗腫瘤功效，通過hjc黄金城使用HCC70模型進行
TAK-243 is a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade. TAK-243 has UAE-specific antitumor efficacy in vivo. Medicilon performed the experiment using the HCC70 (triple-negative breast cancer) model.
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TAK-243是一種有效的泛素激活酶小分子抑製劑，具有體內抗腫瘤功效，通過hjc黄金城使用HCC70模型進行
Jun 28,2023
法尼基轉移酶抑製劑LNK-754單次口服後即可快速穿過血腦屏障，PK分析通過hjc黄金城進行
Pharmacokinetic studies revealed that after a single oral dose, the FTI (LNK-754) was cleared from plasma within 20 hours and could rapidly cross the blood-brain-barrier. Pharmacokinetic analysis was performed as a service provided by Medicilon.
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法尼基轉移酶抑製劑LNK-754單次口服後即可快速穿過血腦屏障，PK分析通過hjc黄金城進行
Jun 28,2023
WYC-209可抑製惡性小鼠黑色素瘤腫瘤再生細胞增殖，SPR分析通過hjc黄金城使用Biacore 8K設備進行
The binding assay by surface plasmon resonance (SPR) analysis shows that WYC-209A and WYC-209B acid bind to RARs at nano-molar doses. SPR was carried out by Medicilon, using the Biacore 8K equipment.
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WYC-209可抑製惡性小鼠黑色素瘤腫瘤再生細胞增殖，SPR分析通過hjc黄金城使用Biacore 8K設備進行
Jun 28,2023
ARD-2128是一種PROTAC AR降解劑，具有出色的血漿和微粒體穩定性，體外穩定性和PK研究通過hjc黄金城進行
ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.
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ARD-2128是一種PROTAC AR降解劑，具有出色的血漿和微粒體穩定性，體外穩定性和PK研究通過hjc黄金城進行
Jun 28,2023
設計合成一係列DHODH抑製劑作為潛在的類風濕性關節炎治療藥物，PK研究通過hjc黄金城進行
Human dihydroorotate dehydrogenase (DHODH) is a viable target for the development of therapeutics to treat cancer and immunological diseases. Herein, researchers designed and synthesized a series of acrylamide-based novel DHODH inhibitors as potential rheumatoid arthritis (RA) treatment agents.
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設計合成一係列DHODH抑製劑作為潛在的類風濕性關節炎治療藥物，PK研究通過hjc黄金城進行