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搜索结果包含 oral bioavailability 的内容

Jul 06,2023
表观遗传修饰,如DNA甲基化,在遗传信息的表达中发挥着重要作用。DNA甲基转移酶维持DNA甲基化,是肿瘤化疗的一个有吸引力的靶点
Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tu
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表观遗传修饰,如DNA甲基化,在遗传信息的表达中发挥着重要作用。DNA甲基转移酶维持DNA甲基化,是肿瘤化疗的一个有吸引力的靶点
Jul 06,2023
ANO1是一个潜在的镇痛靶点。DFBTA是一种有效的ANO1抑制剂,具有优异的药代动力学特性。体内PK测试通过美迪西进行
Current pain management is largely limited to opioids and non-steroidal anti-inflammatory drugs. Developing new analgesic drugs remains important to address the unmet medical needs of chronic pain pat
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ANO1是一个潜在的镇痛靶点。DFBTA是一种有效的ANO1抑制剂,具有优异的药代动力学特性。体内PK测试通过美迪西进行
Jul 06,2023
Y180是一种口服Mpro抑制剂,可有效对抗野生型SARS-CoV-2及其变种。Y180在小鼠、大鼠和狗中具有良好的PK特性
Y180, an orally available Mpro inhibitor, is effective against wild-type SARS-CoV-2 and variants. Y180 displayed satisfying PK properties in mice, rats and dogs, with oral bioavailabilities of 92.9%,
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Y180是一种口服Mpro抑制剂,可有效对抗野生型SARS-CoV-2及其变种。Y180在小鼠、大鼠和狗中具有良好的PK特性
Jul 06,2023
Ulotaront是一种具有5-HT1A激动剂活性的TAAR1 激动剂,可用于治疗精神分裂症。Ulotaront在大鼠脑中的分布和在猴血浆中的PK研究通过美迪西进行
Ulotaront (SEP-363856) is a TAAR1 agonist with 5-HT1A agonist activity currently in clinical development for the treatment of Schizophrenia. Ulotaront exhibits rapid absorption, greater than 70% bioav
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Ulotaront是一种具有5-HT1A激动剂活性的TAAR1 激动剂,可用于治疗精神分裂症。Ulotaront在大鼠脑中的分布和在猴血浆中的PK研究通过美迪西进行
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 p
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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
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. Practi
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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
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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
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
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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
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
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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
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研究通过美迪西进行
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 oncoprotei
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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研究通过美迪西进行
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美迪西进行
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 metho
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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美迪西进行
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) 实验通过美迪西进行
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
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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) 实验通过美迪西进行
Jun 28,2023
法尼基转移酶抑制剂LNK-754单次口服后即可快速穿过血脑屏障,PK分析通过美迪西进行
Pharmacokinetic studies revealed that after a single oral dose, the FTI (LNK-754) was cleared from plasma within 20 hours and could rapidly cross the blood-brain-barrier. Pharmacokinetic analysis was performed as a service provided by Medicilon.
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法尼基转移酶抑制剂LNK-754单次口服后即可快速穿过血脑屏障,PK分析通过美迪西进行
Jun 28,2023
索拉非尼的无定形固体分散体用于开发改良型口服生物利用度高的速释片剂,PK研究通过美迪西进行
The SOR ASD tablets exhibited approximately 50% higher relative bioavailability in dogs than the marketed SOR tablet product, Nexavar®. The pharmacokinetic (PK) study of SOR ASD tablets and Nexavar® tablets was performed by Medicilon.
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索拉非尼的无定形固体分散体用于开发改良型口服生物利用度高的速释片剂,PK研究通过美迪西进行
Jun 28,2023
GS-5801是一种有效的KDM5抑制剂,具有抗HBV活性,GS-5801通过美迪西合成
GS-5801, a potent inhibitor of KDM5, has antiviral activity against HBV in a primary human hepatocytes infection model, with the cellular permeability, oral bioavailability. GS-5801 was synthesized by Medicilon.
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GS-5801是一种有效的KDM5抑制剂,具有抗HBV活性,GS-5801通过美迪西合成
Jun 28,2023
设计合成一种新型选择性的口服有效苏氨酸酪氨酸激酶 (TTK) 抑制剂,PK研究均通过美迪西进行
TTK inhibition is an attractive wide-spectrum strategy for cancer therapy. Researchers designed and synthesized a series of pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable TTK inhibitors. All the pharmacokinetic studies were carrie
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设计合成一种新型选择性的口服有效苏氨酸酪氨酸激酶 (TTK) 抑制剂,PK研究均通过美迪西进行
Jun 28,2023
TR-107是人类线粒体蛋白酶ClpP的有效激活剂,PK分析通过美迪西进行
The pharmacokinetic properties of TR‐107 were compared with other known ClpP activators including ONC201 and ONC212. TR‐107 displayed excellent exposure and serum t1/2 after oral administration. Pharmacokinetic analysis were evalsuated for pharmacokinetic
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TR-107是人类线粒体蛋白酶ClpP的有效激活剂,PK分析通过美迪西进行
Jun 28,2023
JND003是一种新型选择性ERRα激动剂,可缓解非酒精性脂肪肝和胰岛素抵抗,PK和组织分布测定通过美迪西进行
JND003 is orally bioavailable and exhibits high grade of distribution in liver and abdominal adipose tissues. Pharmacokinetics (PK) and Tissue Distribution Assays of JND003 were performed at Medicilon.
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JND003是一种新型选择性ERRα激动剂,可缓解非酒精性脂肪肝和胰岛素抵抗,PK和组织分布测定通过美迪西进行
Oct 16,2015
仿制药质量一致性评价
药物溶出度试验是考察、评价制剂内在质量的重要指标。是考察在生产工艺、制剂配方的重要手段。并作为药物体外-体内相关(invitro-in vivo correlation,IVIVC)、生物等效性(Bioequivalance)与生物有效性(Bioavailability)的评价手段。
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仿制药质量一致性评价
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