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    中國：

    Email: marketing@yakkaa.com

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Jul 05,2023
端錨聚合酶1/2影響WNT/β-連環蛋白和Hippo信號通路，這些信號通路涉及包括腫瘤在內的多種疾病
Tankyrase 1 and 2 (TNKS1/2) impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer. OM-153 shows picomolar IC50 inhibition in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable ADME properties, and an improved pharmacokinetic profile in mice. The pharmacokinetic analyses in mice were performed according to the standard protocols of Medicilon.
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端錨聚合酶1/2影響WNT/β-連環蛋白和Hippo信號通路，這些信號通路涉及包括腫瘤在內的多種疾病
Jul 05,2023
設計合成和評估用於治療前列腺癌的CBP溴結構域抑製劑。PK評估、肝微粒體穩定性測定和Caco-2滲透性測定通過hjc黄金城進行
Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Researchers designed 1-(Indolizin-3-yl)ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer. Pharmacokinetic properties evaluation were analyzed by Medicilon. Liver microsomal stability assay were performed at Medicilon. Caco-2 permeability assay was analyzed by Medicilon.
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設計合成和評估用於治療前列腺癌的CBP溴結構域抑製劑。PK評估、肝微粒體穩定性測定和Caco-2滲透性測定通過hjc黄金城進行
Jul 05,2023
研究人員使用RZ-2994來表征抑製SHMT1/2在T細胞急性淋巴細胞白血病 (T-ALL) 中的作用，RZ-2994通過hjc黄金城定製合成
​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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研究人員使用RZ-2994來表征抑製SHMT1/2在T細胞急性淋巴細胞白血病 (T-ALL) 中的作用，RZ-2994通過hjc黄金城定製合成
Jul 05,2023
研究人員開發了一種高特異性的CDC7抑製劑TAK-931作為臨床腫瘤治療劑，抗腫瘤藥效研究通過hjc黄金城進行
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 evaluation system for preclinical anti-tumor efficacy, and has more than 200 different types of tumor efficacy models.
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研究人員開發了一種高特異性的CDC7抑製劑TAK-931作為臨床腫瘤治療劑，抗腫瘤藥效研究通過hjc黄金城進行
Jul 05,2023
研究新型多靶點抗高血壓藥MT-1207的藥理學特性，評價MT-1207的結合抑製活性通過hjc黄金城進行
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 evaluated by Medicilon.
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研究新型多靶點抗高血壓藥MT-1207的藥理學特性，評價MT-1207的結合抑製活性通過hjc黄金城進行
Jul 05,2023
設計、合成和評估具有體內抗炎活性的RIPK1抑製劑，PK研究通過hjc黄金城進行
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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設計、合成和評估具有體內抗炎活性的RIPK1抑製劑，PK研究通過hjc黄金城進行
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