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Aug 21,2023
TAK-931是一种高效的CDC7抑制剂,通过抑制CDC7来抑制DNA复制,具有抗肿瘤功效,体内药效研究通过美迪西进行
Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell divis
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TAK-931是一种高效的CDC7抑制剂,通过抑制CDC7来抑制DNA复制,具有抗肿瘤功效,体内药效研究通过美迪西进行
Jul 06,2023
TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂,具有良好的Caco-2渗透性。Caco-2 渗透性测定通过美迪西进行
TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers”and potential therapeutic targets for cancer and other diseases. Y0
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TRIM24和BRPF1是癌症的潜在治疗靶点。Y08624是一种新型TRIM24/BRPF1双重抑制剂,具有良好的Caco-2渗透性。Caco-2 渗透性测定通过美迪西进行
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
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
XY153是一种有潜力的先导化合物,可用于开发针对急性髓系白血病。XY153在体外具有良好的代谢稳定性。所有肝微粒体测定均通过美迪西进行
Pan-bromodomain and extra terminal (Pan-BET) inhibitors show profound efficacy but exhibit pharmacology-driven toxicities in clinical trials. The representative Compound 8l (XY153), a novel BD2-select
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XY153是一种有潜力的先导化合物,可用于开发针对急性髓系白血病。XY153在体外具有良好的代谢稳定性。所有肝微粒体测定均通过美迪西进行
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
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
4-正丁基间苯二酚是一种高效的酪氨酸酶抑制剂,可用于化妆品中以达到脱色的目的。其中经皮吸收和皮肤分布研究通过美迪西进行
4-n-butyl resorcinol (4-nBR) is a highly effective tyrosinase inhibitor, and can be used in cosmetic product for depigmentation purpose. Its efficacy correlates with 4-nBR that absorbed by skin. In th
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4-正丁基间苯二酚是一种高效的酪氨酸酶抑制剂,可用于化妆品中以达到脱色的目的。其中经皮吸收和皮肤分布研究通过美迪西进行
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
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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 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实验通过美迪西进行
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
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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实验通过美迪西进行
Jul 05,2023
阿帕替尼通过VEGFR2通路抑制紫杉醇对胃癌细胞的耐药性
Overexpression of VEGFR2 can offset the rescue effect of Apatinib on Paclitaxel-induced drug resistance of MGC803 cells. Apatinib inhibits Paclitaxel resistance of MGC803 cells via the VEGFR2 #signali
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阿帕替尼通过VEGFR2通路抑制紫杉醇对胃癌细胞的耐药性
Jul 05,2023
RIPK2激酶参与多种慢性炎症,UH15-15抑制RIPK2激酶并具有良好的体外ADME和PK特性,PK研究通过美迪西进行
Receptor interacting protein kinase-2 (#RIPK2) is an enzyme involved in the transduction of pro-inflammatory nucleotide-binding oligomerization domain cell signaling, a pathway implicated in numerous
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RIPK2激酶参与多种慢性炎症,UH15-15抑制RIPK2激酶并具有良好的体外ADME和PK特性,PK研究通过美迪西进行
Jul 05,2023
SLL-1206是一种κ阿片受体激动剂,具有显著改善的理化和药代动力学特性。作者感谢美迪西对SLL-1206进行的药代动力学研究
The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar acti
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SLL-1206是一种κ阿片受体激动剂,具有显著改善的理化和药代动力学特性。作者感谢美迪西对SLL-1206进行的药代动力学研究
Jul 05,2023
苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中,所有肝微粒体测定均通过美迪西进行
Receptor-related orphan receptor γ (RORγ) has emerged as an attractive therapeutic target for the treatment of cancer and inflammatory diseases. XY123 potently inhibits the RORγ transcription activity
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苯并咪唑衍生物XY123是一种口服有效的选择性RORγ反向激动剂。在本研究中,所有肝微粒体测定均通过美迪西进行
Jul 05,2023
zapERtrap:光调节的内质网释放系统揭示了意想不到的神经元运输途径,Zapalog的合成通过美迪西进行
zapERtrap opens the door to previously unapproachable questions concerning how proteins are processed, trafficked, and secreted in space and time in complex cellular environments. zapERtrap relies on
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zapERtrap:光调节的内质网释放系统揭示了意想不到的神经元运输途径,Zapalog的合成通过美迪西进行
Jul 05,2023
研究新型多靶点抗高血压药MT-1207的药理学特性,评价MT-1207的结合抑制活性通过美迪西进行
Hypertension is a serious public health problem worldwide. MT-1207 is a chemical entity that has entered into clinical trial as antihypertensive agent. MT-1207 potently inhibits adrenergic α1A, α1B, α
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研究新型多靶点抗高血压药MT-1207的药理学特性,评价MT-1207的结合抑制活性通过美迪西进行
Jul 05,2023
ARD-2585是一种口服有效的PROTAC雄激素受体降解剂,可用于治疗晚期前列腺癌。肝微粒体稳定性测定、血浆稳定性测定和hERG测定通过美迪西进行
A PROTAC-based androgen receptor (AR) degrader is a bifunctional small molecule, consisting of an AR ligand that binds to AR protein, and a ligand that binds to and recruits an E3 ligase complex, teth
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ARD-2585是一种口服有效的PROTAC雄激素受体降解剂,可用于治疗晚期前列腺癌。肝微粒体稳定性测定、血浆稳定性测定和hERG测定通过美迪西进行
Jun 28,2023
SAHA可有效恢复阿尔茨海默病模型的记忆能力,本研究中SAHA通过美迪西合成
SAHA was synthesized by Medicilon and was given to mice as 50 mg/kg doses. Injections (10 mL/kg) were given intraperitoneally and were alternated daily between left and right sides of the abdomen. Chronic treatments of SAHA completely restored performance
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SAHA可有效恢复阿尔茨海默病模型的记忆能力,本研究中SAHA通过美迪西合成
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