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Jul 05,2023
设计、合成和评估具有体内抗炎活性的RIPK1抑制剂，PK研究通过s36沙龙会进行
RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).
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设计、合成和评估具有体内抗炎活性的RIPK1抑制剂，PK研究通过s36沙龙会进行
Jul 05,2023
合成一类新型选择性TNIK抑制剂并评估其抗结直肠癌作用，PK研究通过s36沙龙会进行
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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合成一类新型选择性TNIK抑制剂并评估其抗结直肠癌作用，PK研究通过s36沙龙会进行
Jul 05,2023
用于治疗非酒精性脂肪性肝炎的PPARα/δ 双重激动剂的设计合成和生物学评价，PK研究、hERG研究和Ames试验通过s36沙龙会进行
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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用于治疗非酒精性脂肪性肝炎的PPARα/δ 双重激动剂的设计合成和生物学评价，PK研究、hERG研究和Ames试验通过s36沙龙会进行
Jul 05,2023
ARD-2585是一种口服有效的PROTAC雄激素受体降解剂，可用于治疗晚期前列腺癌。肝微粒体稳定性测定、血浆稳定性测定和hERG测定通过s36沙龙会进行
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是一种口服有效的PROTAC雄激素受体降解剂，可用于治疗晚期前列腺癌。肝微粒体稳定性测定、血浆稳定性测定和hERG测定通过s36沙龙会进行
Jul 05,2023
选择性小分子c-Myc降解剂可有效消退c-Myc过表达的肿瘤，表面等离子共振 (SPR) 实验通过s36沙龙会进行
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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选择性小分子c-Myc降解剂可有效消退c-Myc过表达的肿瘤，表面等离子共振 (SPR) 实验通过s36沙龙会进行
Jun 28,2023
SAHA可有效恢复阿尔茨海默病模型的记忆能力，本研究中SAHA通过s36沙龙会合成
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可有效恢复阿尔茨海默病模型的记忆能力，本研究中SAHA通过s36沙龙会合成
Jun 28,2023
TAK-243是一种有效的泛素激活酶小分子抑制剂，具有体内抗肿瘤功效，通过s36沙龙会使用HCC70模型进行
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是一种有效的泛素激活酶小分子抑制剂，具有体内抗肿瘤功效，通过s36沙龙会使用HCC70模型进行
Jun 28,2023
法尼基转移酶抑制剂LNK-754单次口服后即可快速穿过血脑屏障，PK分析通过s36沙龙会进行
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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法尼基转移酶抑制剂LNK-754单次口服后即可快速穿过血脑屏障，PK分析通过s36沙龙会进行
Jun 28,2023
WYC-209可抑制恶性小鼠黑色素瘤肿瘤再生细胞增殖，SPR分析通过s36沙龙会使用Biacore 8K设备进行
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可抑制恶性小鼠黑色素瘤肿瘤再生细胞增殖，SPR分析通过s36沙龙会使用Biacore 8K设备进行
Jun 28,2023
ARD-2128是一种PROTAC AR降解剂，具有出色的血浆和微粒体稳定性，体外稳定性和PK研究通过s36沙龙会进行
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是一种PROTAC AR降解剂，具有出色的血浆和微粒体稳定性，体外稳定性和PK研究通过s36沙龙会进行
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