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Jul 05,2023
研究人员使用RZ-2994来表征抑制SHMT1/2在T细胞急性淋巴细胞白血病 (T-ALL) 中的作用，RZ-2994通过z6尊龙定制合成
​Despite progress in the treatment of T-cell acute lymphoblastic leukemia (T-ALL) has limited treatment options, particularly in the setting of relapsed/refractory disease. Researchers used SHMT1/2 inhibitor RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. Loss of both SHMT1/2 is necessary for impaired growth and cell cycle arrest, with suppression of SHMT1/2 inhibiting leukemia progression. RZ-2994 also decreases leukemia burden in vivo. RZ-2994 was obtained from Medicilon. Medicilon offers a full range of chemical services covering all phases of your project. Customers can work with us either through FFS or FTE.
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研究人员使用RZ-2994来表征抑制SHMT1/2在T细胞急性淋巴细胞白血病 (T-ALL) 中的作用，RZ-2994通过z6尊龙定制合成
Jul 05,2023
研究人员开发了一种高特异性的CDC7抑制剂TAK-931作为临床肿瘤治疗剂，抗肿瘤药效研究通过z6尊龙进行
Cell division cycle 7 (CDC7) plays important roles in DNA replication. Researchers developed a highly specific CDC7 inhibitor, TAK-931, as a clinical cancer therapeutic agent. The antitumor efficacy studies in PDX models were performed at Medicilon. Medicilon has established a complete evalsuation system for preclinical anti-tumor efficacy, and has more than 200 different types of tumor efficacy models.
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研究人员开发了一种高特异性的CDC7抑制剂TAK-931作为临床肿瘤治疗剂，抗肿瘤药效研究通过z6尊龙进行
Jul 05,2023
研究新型多靶点抗高血压药MT-1207的药理学特性，评价MT-1207的结合抑制活性通过z6尊龙进行
Hypertension is a serious public health problem worldwide. MT-1207 is a chemical entity that has entered into clinical trial as antihypertensive agent. MT-1207 potently inhibits adrenergic α1A, α1B, α1D, and 5-HT2A receptors with Ki<1 nM in a panel of enzyme activity or radioligand binding assays. The binding inhibition activities of MT-1207 were evalsuated by Medicilon.
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研究新型多靶点抗高血压药MT-1207的药理学特性，评价MT-1207的结合抑制活性通过z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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 biosesensor 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z6尊龙进行
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z6尊龙合成
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z6尊龙合成
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z6尊龙使用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z6尊龙使用HCC70模型进行
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