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搜索结果包含 pharmacokinetic 的内容

Jul 06,2023
发现新型RAGE/SERT双重抑制剂,可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托美迪西进行
Alzheimer's disease (AD) is a progressive and devastating neurodegenerative disorder, characterized by the presence of β-amyloid (Aβ) peptide plaques, neurofibrillary tangles, and neuroinflammatio
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发现新型RAGE/SERT双重抑制剂,可用于治疗阿尔茨海默病和抑郁症。其中药代动力学研究是通过委托美迪西进行
Jul 06,2023
IAP蛋白是有吸引力的癌症治疗靶点。SM-406 是一种口服有效的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过美迪西进行
Apoptosis is a cellular process critical to the normal development and homeostasis of multicellular organisms. The inhibitor of apoptosis proteins (IAPs) are a class of key apoptosis regulators.
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IAP蛋白是有吸引力的癌症治疗靶点。SM-406 是一种口服有效的IAP拮抗剂。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通过美迪西进行
Jul 06,2023
设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂,并进行生物学评价。其中药代动力学分析通过美迪西进行
Gastric cancer is the second most lethal cancer across the world. Compounds 8f, inhibits FGFR1 signaling pathways as well as induces cell apoptosis, is a potential agent for the treatment of gastric c
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设计合成一系列用于治疗胃癌的多靶点受体酪氨酸激酶抑制剂,并进行生物学评价。其中药代动力学分析通过美迪西进行
Jul 06,2023
FBPase是与肿瘤和2型糖尿病相关的一个有前景的靶点。化合物W8对FBPase表现出高选择性。W8的药代动力学研究通过美迪西进行
Fructose-1,6-bisphosphatase (FBPase) is a promising target associated with cancer and type 2 diabetes. Compounds W8 and W8k exhibit high selectivity against FBPase and W8 effectively reduces blood glu
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FBPase是与肿瘤和2型糖尿病相关的一个有前景的靶点。化合物W8对FBPase表现出高选择性。W8的药代动力学研究通过美迪西进行
Jul 06,2023
药物发现中的挑战之一是识别高质量的先导化合物。此研究中PK结果表明L12可作为针对PDE5的先导化合物,进一步研究和开发。L12的PK分析通过美迪西进行
Scaffold hopping refers to computer-aided screening for active compounds with different structures against the same receptor to enrich privileged scaffolds, which is a topic of high interest in organi
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药物发现中的挑战之一是识别高质量的先导化合物。此研究中PK结果表明L12可作为针对PDE5的先导化合物,进一步研究和开发。L12的PK分析通过美迪西进行
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
开发和验证大鼠血浆中Nobiliside A定量的LC/MS/MS方法
Nobiliside A, a new triterpene glycoside, exhibits some biological activities including antifungal and cytotoxic effects. A LC/MS/MS method was developed and validated for determination of Nobiliside
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开发和验证大鼠血浆中Nobiliside A定量的LC/MS/MS方法
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,
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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. 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
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 p
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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
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
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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
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
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
ARD-2128是一种PROTAC AR降解剂,具有出色的血浆和微粒体稳定性,体外稳定性和PK研究通过美迪西进行
ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.
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ARD-2128是一种PROTAC AR降解剂,具有出色的血浆和微粒体稳定性,体外稳定性和PK研究通过美迪西进行
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
QF-036是一种高效的HIV-1抑制剂,具有良好的和药代动力学特性,PK研究通过美迪西进行
The favourable viral inhibitory activity and pharmacokinetic properties provide critical support for QF-036 as a promising anti-HIV therapeutic candidate. The pharmacokinetic studies were performed by Medicilon.
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QF-036是一种高效的HIV-1抑制剂,具有良好的和药代动力学特性,PK研究通过美迪西进行
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
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