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Jul 06,2023
以PROTAC為代表的靶向蛋白質降解是藥物發現的新興策略，研究人員設計並合成了多種PROTAC，此研究中所有PK研究均通過hjc黄金城進行
Targeted protein degradation (TPD) exemplified by PROTACs is an emerging strategy for next generation drug discovery. Threonine tyrosine kinase (TTK) is a dual-specific protein kinase that catalyzes phosphorylation of both serine/threonine and tyrosine residues. Researchers designed and synthesized TTK PROTACs, which demonstrated reasonable pharmacokinetic profiles. All the pharmacokinetic studies were carried out by Medicilon, according to the protocols and guidelines of the institutional care and use committee.
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以PROTAC為代表的靶向蛋白質降解是藥物發現的新興策略，研究人員設計並合成了多種PROTAC，此研究中所有PK研究均通過hjc黄金城進行
Jul 06,2023
氯磺丙脲對蠕蟲和人肺成纖維細胞MRC-5細胞具有抗衰老作用，氯磺丙脲在小鼠中的生物利用度測定通過hjc黄金城進行
Sulfonylureas exert their anti-diabetic effects by inhibiting K-ATP channels in the plasma membrane of islet β-cells. Chlorpropamide acts on complex II directly or indirectly via mitoK-ATP to produce mtROS as a pro-longevity signal. Chlorpropamide has an anti-aging effect on worms and human lung fibroblast MRC-5 cells. Determination of Chlorpropamide bioavailability in mice was performed by Medicilon.
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氯磺丙脲對蠕蟲和人肺成纖維細胞MRC-5細胞具有抗衰老作用，氯磺丙脲在小鼠中的生物利用度測定通過hjc黄金城進行
Jul 06,2023
BRD4抑製劑可用於治療腎纖維化，ZLD2218可有效抑製BRD4活性，對ZLD2218的PK研究通過hjc黄金城進行
Uncovering new therapeutics for kidney fibrosis hold promise for chronic kidney disease (CKD). BRD4 inhibition ameliorated kidney injury and fibrosis. ZLD2218 exhibited the potent inhibitory activity against BRD4, with the IC50 value of 107 nM. Pharmacokinetic analysis of of ZLD2218 were analyzed by noncompartmental methods using Phoenix WinNonlin 7.0 (Accomplished by Medicilon).
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BRD4抑製劑可用於治療腎纖維化，ZLD2218可有效抑製BRD4活性，對ZLD2218的PK研究通過hjc黄金城進行
Jul 06,2023
免疫檢查點阻斷療法改變了癌症治療的範式，此研究中通過hjc黄金城在23 個同源腫瘤模型中進行了抗PD-1抗體的體內研究
Immune checkpoint blockade therapies have changed the paradigm of cancer therapies. Reseachers performed in vivo screening for anti-PD-1 therapy across 23 syngeneic tumor models and found that CT-26 and Colon 26, which are murine colorectal carcinoma derived from BALB/c mice, showed different sensitivity to anti-PD-1. In vivo studies for anti-PD-1 antibody across 23 syngeneic tumor models were performed by Medicilon.
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免疫檢查點阻斷療法改變了癌症治療的範式，此研究中通過hjc黄金城在23 個同源腫瘤模型中進行了抗PD-1抗體的體內研究
Jul 06,2023
PDE1是與中樞和外周疾病密切相關的藥物靶點，研究人員合成一種PDE1 抑製劑在大鼠肝微粒體中具有良好的代謝穩定性。其中穩定性測試通過hjc黄金城進行
Phosphodiesterase-1 (PDE1) is a promising drug target closely related to central and peripheral diseases. Compound 2j with the IC50 of 21 nM against PDE1B, shows good metabolic stability in the rat liver microsomes. Stability test in the rat liver microsomes were performed by Medicilon.
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PDE1是與中樞和外周疾病密切相關的藥物靶點，研究人員合成一種PDE1 抑製劑在大鼠肝微粒體中具有良好的代謝穩定性。其中穩定性測試通過hjc黄金城進行
Jul 06,2023
SKLB-YTH-60可改善博來黴素誘導的肺纖維化小鼠模型中的炎症和纖維化，YTH-60的體內藥代動力學研究通過hjc黄金城進行
Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through computer-aided drug design, de novo synthesis and high-throughput screening. YTH-60 has obvious anti‐proliferative activity on fibroblasts and A549 cells. YTH-60 has an acceptable oral bioavailability and appropriate eliminated half-life time. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon.
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SKLB-YTH-60可改善博來黴素誘導的肺纖維化小鼠模型中的炎症和纖維化，YTH-60的體內藥代動力學研究通過hjc黄金城進行
Jul 06,2023
研究人員成功發現了一種口服PROTAC降解劑SIAIS164018，具有良好的體內耐受性。PK和MTD研究通過hjc黄金城進行
PROTAC is an attractive technology in drug discovery. Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 which degrades not only ALK or mutant EGFR but also oncoproteins involved in metastasis. SIAIS164018 is orally bioavailable and well tolerated in vivo. Pharmacokinetic and maximal tolerated dose (MTD) assays were performed by Medicilon.
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研究人員成功發現了一種口服PROTAC降解劑SIAIS164018，具有良好的體內耐受性。PK和MTD研究通過hjc黄金城進行
Jul 06,2023
開發具有口服活性的高度選擇性卵泡刺激激素受體激動劑，且進行臨床前研究。其中對大鼠和狗的毒理學評估通過hjc黄金城進行
TOP5300 is an orally active follicle stimulating hormone receptor allosteric agonist that provides a preferred treatment for over 16 million infertile women of reproductive age in low complexity methods or in high complexity methods. TOP5300 was evaluated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evaluations were performed in both rat and dog as the second species according to the guidance from FDA. These assays were performed by Medicilon.
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開發具有口服活性的高度選擇性卵泡刺激激素受體激動劑，且進行臨床前研究。其中對大鼠和狗的毒理學評估通過hjc黄金城進行
Jul 06,2023
PARP1/2抑製劑有治療腫瘤的潛力，PARP1/2抑製實驗通過hjc黄金城進行
Poly ADP-ribose polymerases (PARPs) are a family of enzymes related to DNA damage repair process. Inhibition of PARP1/2 accelerates the damage of injured DNA, which is synthetically lethal to DNA-repairing-deficient cancer cells, such as BRCA1/2-deficient cells. PARP1/2 inhibitors could be a promising candidate for the treatment of cancer. The PARP1 and PARP2 inhibition assays were performed by Medicilon.
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PARP1/2抑製劑有治療腫瘤的潛力，PARP1/2抑製實驗通過hjc黄金城進行
Jul 06,2023
使用hjc黄金城硒代氨基酸培養基產品發表的學術文獻
hjc黄金城提供全套M9硒代蛋氨酸（SeMET）培養基，可用於IPTG誘導的大腸杆菌表達係統，生產硒代蛋氨酸標記的蛋白，運用多波長反常散射（MAD）方法進行蛋白質晶體學研究。
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使用hjc黄金城硒代氨基酸培養基產品發表的學術文獻