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Jul 02,2025
口服有效的ADAMTS-4/5抑制劑異吲哚啉酰胺衍生物，可治療骨關節炎，本研究中部分化合物通過尊龍凱時合成
Part of the compound synthesis was performed at Medicilon.
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Jun 12,2025
新型5-HT3受體配體有望用于治療神經精神疾病和胃腸道疾病，本研究中藥理藥效學研究通過尊龍凱時進行
The experiments (Rat colon distension model of IBS-d) were carried out by Medicilon. The protocol complied with and was approved by the Institutional Animal Care and Use Committee and Medicilon is accredited by the NIH Office of laboratory Animal Welfare
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Aug 21,2023
TAK-931是一種高效的CDC7抑制劑，通過抑制CDC7來抑制DNA復制，具有抗腫瘤功效，體內藥效研究通過尊龍凱時進行
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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Jul 06,2023
TRIM24和BRPF1是癌癥的潛在治療靶點。Y08624是一種新型TRIM24/BRPF1雙重抑制劑，具有良好的Caco-2滲透性。Caco-2 滲透性測定通過尊龍凱時進行
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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Jul 06,2023
IAP蛋白是有吸引力的癌癥治療靶點。SM-406 是一種口服有效的IAP拮抗劑。SM-406 在雄性SD大鼠、比格犬和NHP中的PK研究通過尊龍凱時進行
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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Jul 06,2023
設計合成一系列用于治療胃癌的多靶點受體酪氨酸激酶抑制劑，并進行生物學評價。其中藥代動力學分析通過尊龍凱時進行
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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Jul 06,2023
表觀遺傳修飾，如DNA甲基化，在遺傳信息的表達中發揮著重要作用。DNA甲基轉移酶維持DNA甲基化，是腫瘤化療的一個有吸引力的靶點
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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Jul 06,2023
Y180是一種口服Mpro抑制劑，可有效對抗野生型SARS-CoV-2及其變種。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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Jul 06,2023
Ulotaront是一種具有5-HT1A激動劑活性的TAAR1 激動劑，可用于治療精神分裂癥。Ulotaront在大鼠腦中的分布和在猴血漿中的PK研究通過尊龍凱時進行
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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Jul 06,2023
開發和驗證大鼠血漿中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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Jul 06,2023
4-正丁基間苯二酚是一種高效的酪氨酸酶抑制劑，可用于化妝品中以達到脫色的目的。其中經皮吸收和皮膚分布研究通過尊龍凱時進行
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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Jul 06,2023
氯磺丙脲對蠕蟲和人肺成纖維細胞MRC-5細胞具有抗衰老作用，氯磺丙脲在小鼠中的生物利用度測定通過尊龍凱時進行
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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Jul 05,2023
研究人員設計合成STAT3和HDAC雙通路抑制劑用于治療實體腫瘤，PK實驗通過尊龍凱時進行
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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Jul 05,2023
阿帕替尼通過VEGFR2通路抑制紫杉醇對胃癌細胞的耐藥性
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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Jul 05,2023
SLL-1206是一種κ阿片受體激動劑，具有顯著改善的理化和藥代動力學特性。作者感謝尊龍凱時對SLL-1206進行的藥代動力學研究
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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Jul 05,2023
苯并咪唑衍生物XY123是一種口服有效的選擇性RORγ反向激動劑。在本研究中，所有肝微粒體測定均通過尊龍凱時進行
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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Jul 05,2023
zapERtrap：光調節的內質網釋放系統揭示了意想不到的神經元運輸途徑，Zapalog的合成通過尊龍凱時進行
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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Jul 05,2023
研究新型多靶點抗高血壓藥MT-1207的藥理學特性，評價MT-1207的結合抑制活性通過尊龍凱時進行
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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Jul 05,2023
ARD-2585是一種口服有效的PROTAC雄激素受體降解劑，可用于治療晚期前列腺癌。肝微粒體穩定性測定、血漿穩定性測定和hERG測定通過尊龍凱時進行
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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Jun 28,2023
SAHA可有效恢復阿爾茨海默病模型的記憶能力，本研究中SAHA通過尊龍凱時合成
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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