Jul 05,2023

用于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試驗通過尊龍凱時進行

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.

Jul 05,2023

ARD-2585是一種口服有效的PROTAC雄激素受體降解劑，可用于治療晚期前列腺癌。肝微粒體穩定性測定、血漿穩定性測定和hERG測定通過尊龍凱時進行

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.

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，表面等離子共振 (SPR) 實驗通過尊龍凱時進行

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.

Jun 28,2023

SAHA可有效恢復阿爾茨海默病模型的記憶能力，本研究中SAHA通過尊龍凱時合成

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.

Jun 28,2023

TAK-243是一種有效的泛素激活酶小分子抑制劑，具有體內抗腫瘤功效，通過尊龍凱時使用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.

Jun 28,2023

法尼基轉移酶抑制劑LNK-754單次口服后即可快速穿過血腦屏障，本研究中PK分析通過尊龍凱時進行

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.

Jun 28,2023

WYC-209可抑制惡性小鼠黑色素瘤腫瘤再生細胞增殖，本研究中SPR通過尊龍凱時使用Biacore 8K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.

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，本研究中體外穩定性和PK研究通過尊龍凱時進行

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.

Jun 28,2023

設計合成一系列DHODH抑制劑作為潛在的類風濕性關節炎治療藥物，本研究中PK實驗通過尊龍凱時進行

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.

Jun 28,2023

開發并驗證新的LC-MS/MS方法，用于定量人血漿中達拉非尼及其主要代謝物羥基達拉非尼 (OHD)。本研究中OHD(純度>99%)通過尊龍凱時合成

OHD (purity >99 %) was synthesized by Medicilon. Medicilon synthetic chemistry team is capable of the independent design of synthesis pathways and complex compound treatments, key to helping accelerate drug discovery.