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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z6尊龙进行
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z6尊龙进行
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z6尊龙在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z6尊龙在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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
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z6尊龙进行
Jul 06,2023
研究人员成功发现了一种口服PROTAC降解剂SIAIS164018,具有良好的体内耐受性。PK和MTD研究通过z6尊龙进行
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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研究人员成功发现了一种口服PROTAC降解剂SIAIS164018,具有良好的体内耐受性。PK和MTD研究通过z6尊龙进行
Jul 06,2023
开发具有口服活性的高度选择性卵泡刺激激素受体激动剂,且进行临床前研究。其中对大鼠和狗的毒理学评估通过z6尊龙进行
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 evalsuated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evalsuations 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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开发具有口服活性的高度选择性卵泡刺激激素受体激动剂,且进行临床前研究。其中对大鼠和狗的毒理学评估通过z6尊龙进行
Jul 06,2023
PARP1/2抑制剂有治疗肿瘤的潜力,PARP1/2抑制实验通过z6尊龙进行
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抑制剂有治疗肿瘤的潜力,PARP1/2抑制实验通过z6尊龙进行
Jul 06,2023
使用z6尊龙硒代氨基酸培养基产品发表的学术文献
z6尊龙提供全套M9硒代蛋氨酸(SeMET)培养基,可用于IPTG诱导的大肠杆菌表达系统,生产硒代蛋氨酸标记的蛋白,运用多波长反常散射(MAD)方法进行蛋白质晶体学研究。
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使用z6尊龙硒代氨基酸培养基产品发表的学术文献
Jul 05,2023
设计合成一种高度选择性的H435R突变敏感的甲状腺激素受体β激动剂,PK分析通过z6尊龙进行
Thyroid hormone receptors (TRs) are ligand-dependent transcription factors that belong to the nuclear receptor superfamily and also participate in important physiological functions. In this study, Compound 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH). Compound 16g showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. PK properties of Compound 16g were analyzed by Medicilon.
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设计合成一种高度选择性的H435R突变敏感的甲状腺激素受体β激动剂,PK分析通过z6尊龙进行
Jul 05,2023
研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤,PK实验通过z6尊龙进行
The inhibition of HDACs will lead to compensated activation of a notorious cancer-related drug target, STAT3, in breast cancer through a cascade, which probably limits the anti-proliferation effect of HDAC inhibitors in solid tumors. Herein, researchers synthesized a series of potent pterostilbene hydroxamic acid derivatives with dual-target inhibition activity. The pharmacokinetic experiment in SD Rats was carried out by Medicilon.
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研究人员设计合成STAT3和HDAC双通路抑制剂用于治疗实体肿瘤,PK实验通过z6尊龙进行
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