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Jul 06,2023
Columbin具有多种药理活性,包括体内抗炎和抗肿瘤活性,此实验中动物研究通过美迪西进行
Columbin is an important component isolated from Radix Tinosporae. Columbin possesses many pharmacological activities, including anti-inflammation, and antitumor activity in vivo. The purpose of the present study was to examine in vivo pharmacokinetics and bioavailability of Columbin in rats using a high-performance liquid chromatography coupled with tandem mass spectrometry quantitative detection method. This is the first study demonstrating the bioanalytical method and pharmacokinetic of Columbin. Animal studies were carried out in Medicilon.
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Columbin具有多种药理活性,包括体内抗炎和抗肿瘤活性,此实验中动物研究通过美迪西进行
Jul 06,2023
PTX-HSN是一种高效纳米系统,具有较高耐受剂量,可将PTX递送至卵巢癌并增强主动肿瘤靶向性。此研究中所有体内实验均通过美迪西进行
Paclitaxel-loaded hyaluronan solid nanoemulsions (PTX-HSNs) were successfully fabricated for the delivery of PTX to improve ovarian cancer treatment via active tumor targeting. The in vivo toxicity, in vivo antitumor effects, and pharmacokinetics of PTX-HSNs and Taxol were evalsuated in nude mice and rats. PTX-HSN is a highly effective nanosystem with a high maximum tolerated dose (MTD) for delivering PTX to ovarian cancers characterized by CD44 overexpression, enhanced active tumor targeting, and low toxicity. All in vivo experiments were conducted with the approval of the Association for Assessment and Accreditation of Laboratory Animal Care (AAALAC) International (tested at Medicilon/MPI Preclinical Research).
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PTX-HSN是一种高效纳米系统,具有较高耐受剂量,可将PTX递送至卵巢癌并增强主动肿瘤靶向性。此研究中所有体内实验均通过美迪西进行
Jul 06,2023
开发一种简单准确的液相色谱串联质谱法,用于大鼠血浆中牡荆素鼠李糖苷的测定和体内PK研究。此研究中动物研究通过美迪西进行
A simple and accurate liquid chromatography coupled with tandem mass spectrometry method was developed for determination and in vivo pharmacokinetic studies of vitexin rhamnoside in rat plasma. Practical utility of this new LC/MS/MS method was confirmed in pilot pharmacokinetic studies in rats following both intravenous and oral administration. Animal studies were carried out in Medicilon.
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开发一种简单准确的液相色谱串联质谱法,用于大鼠血浆中牡荆素鼠李糖苷的测定和体内PK研究。此研究中动物研究通过美迪西进行
Jul 06,2023
AD80是一种多激酶抑制剂,在多种肝细胞癌临床前动物模型中具有抗肿瘤活性,AD80在血浆中的含量通过美迪西进行LC-MS/MS测定
Liver cancer is the fourth greatest cause of cancer related mortality. AD80 is a multi-kinase inhibitor with anti-tumoral activity across a variety of hepatocellular carcinoma (HCC) preclinical models, including mouse xenografts. AD80 is highly active in a tumor xenograft model. Experimental dosing for AD80 was determined from maximum tolerated dosage (MTD) studies and pharmacokinetic (PK) analysis. Quantities of AD80 in blood plasma were determined by LC-MS/MS at Medicilon.
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AD80是一种多激酶抑制剂,在多种肝细胞癌临床前动物模型中具有抗肿瘤活性,AD80在血浆中的含量通过美迪西进行LC-MS/MS测定
Jul 06,2023
以PROTAC为代表的靶向蛋白质降解是药物发现的新兴策略,研究人员设计并合成了多种PROTAC,此研究中所有PK研究均通过美迪西进行
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为代表的靶向蛋白质降解是药物发现的新兴策略,研究人员设计并合成了多种PROTAC,此研究中所有PK研究均通过美迪西进行
Jul 06,2023
氯磺丙脲对蠕虫和人肺成纤维细胞MRC-5细胞具有抗衰老作用,氯磺丙脲在小鼠中的生物利用度测定通过美迪西进行
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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氯磺丙脲对蠕虫和人肺成纤维细胞MRC-5细胞具有抗衰老作用,氯磺丙脲在小鼠中的生物利用度测定通过美迪西进行
Jul 06,2023
BRD4抑制剂可用于治疗肾纤维化,ZLD2218可有效抑制BRD4活性,对ZLD2218的PK研究通过美迪西进行
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抑制剂可用于治疗肾纤维化,ZLD2218可有效抑制BRD4活性,对ZLD2218的PK研究通过美迪西进行
Jul 06,2023
免疫检查点阻断疗法改变了癌症治疗的范式,此研究中通过美迪西在23 个同源肿瘤模型中进行了抗PD-1抗体的体内研究
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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免疫检查点阻断疗法改变了癌症治疗的范式,此研究中通过美迪西在23 个同源肿瘤模型中进行了抗PD-1抗体的体内研究
Jul 06,2023
PDE1是与中枢和外周疾病密切相关的药物靶点,研究人员合成一种PDE1 抑制剂在大鼠肝微粒体中具有良好的代谢稳定性。其中稳定性测试通过美迪西进行
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是与中枢和外周疾病密切相关的药物靶点,研究人员合成一种PDE1 抑制剂在大鼠肝微粒体中具有良好的代谢稳定性。其中稳定性测试通过美迪西进行
Jul 06,2023
SKLB-YTH-60可改善博来霉素诱导的肺纤维化小鼠模型中的炎症和纤维化,YTH-60的体内药代动力学研究通过美迪西进行
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可改善博来霉素诱导的肺纤维化小鼠模型中的炎症和纤维化,YTH-60的体内药代动力学研究通过美迪西进行
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