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Jul 05,2023
合成具有体内抗肿瘤活性的强效PD-L1抑制剂,并进行生物学评价和机制研究。PK研究通过永乐高进行
PD-1 and PD-L1 have been very successful for the treatment of various tumors, including NSCLC, urothelial cancer, melanoma, head and neck squamous cell cancer, and lymphoma. Researchers identified compound L7 as a potent PD-L1 inhibitor that blocked PD-1/PD-L1 interaction. Pharmacokinetic (PK) studies demonstrated that L7 was orally bioavailable. PK studies were conducted by Medicilon.
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合成具有体内抗肿瘤活性的强效PD-L1抑制剂,并进行生物学评价和机制研究。PK研究通过永乐高进行
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。作者感谢永乐高对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 activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects. The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.
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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。作者感谢永乐高对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永乐高进行
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 with an IC50 value of 64 nM. XY123 demonstrates good metabolic stability and a pharmacokinetics property with reasonable oral bioavailability (32.41%) and moderate half-life (4.98 h). All liver microsome assays were performed by Medicilon.
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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永乐高进行
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的合成通过永乐高进行
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 a small-molecule protein dimerizer zapalog, which consists of the antibiotic trimethoprim tethered to a synthetic ligand of FK506-binding protein through a photocleavable linker. Synthesis of zapalog was performed by Medicilon.
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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的合成通过永乐高进行
Jul 05,2023
端锚聚合酶1/2影响WNT/β-连环蛋白和Hippo信号通路,这些信号通路涉及包括肿瘤在内的多种疾病
Tankyrase 1 and 2 (TNKS1/2) impact the WNT/β-catenin and Hippo signaling pathways that are involved in numerous human disease conditions including cancer. OM-153 shows picomolar IC50 inhibition in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable ADME properties, and an improved pharmacokinetic profile in mice. The pharmacokinetic analyses in mice were performed according to the standard protocols of Medicilon.
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端锚聚合酶1/2影响WNT/β-连环蛋白和Hippo信号通路,这些信号通路涉及包括肿瘤在内的多种疾病
Jul 05,2023
设计合成和评估用于治疗前列腺癌的CBP溴结构域抑制剂。PK评估、肝微粒体稳定性测定和Caco-2渗透性测定通过永乐高进行
Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Researchers designed 1-(Indolizin-3-yl)ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer. Pharmacokinetic properties evaluation were analyzed by Medicilon. Liver microsomal stability assay were performed at Medicilon. Caco-2 permeability assay was analyzed by Medicilon.
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设计合成和评估用于治疗前列腺癌的CBP溴结构域抑制剂。PK评估、肝微粒体稳定性测定和Caco-2渗透性测定通过永乐高进行
Jul 05,2023
研究人员使用RZ-2994来表征抑制SHMT1/2在T细胞急性淋巴细胞白血病 (T-ALL) 中的作用,RZ-2994通过永乐高定制合成
​Despite progress in the treatment of T-cell acute lymphoblastic leukemia (T-ALL) has limited treatment options, particularly in the setting of relapsed/refractory disease. Researchers used SHMT1/2 inhibitor RZ-2994 to characterize the effect of inhibiting SHMT1/2 in T-ALL. Loss of both SHMT1/2 is necessary for impaired growth and cell cycle arrest, with suppression of SHMT1/2 inhibiting leukemia progression. RZ-2994 also decreases leukemia burden in vivo. RZ-2994 was obtained from Medicilon. Medicilon offers a full range of chemical services covering all phases of your project. Customers can work with us either through FFS or FTE.
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研究人员使用RZ-2994来表征抑制SHMT1/2在T细胞急性淋巴细胞白血病 (T-ALL) 中的作用,RZ-2994通过永乐高定制合成
Jul 05,2023
研究人员开发了一种高特异性的CDC7抑制剂TAK-931作为临床肿瘤治疗剂,抗肿瘤药效研究通过永乐高进行
Cell division cycle 7 (CDC7) plays important roles in DNA replication. Researchers developed a highly specific CDC7 inhibitor, TAK-931, as a clinical cancer therapeutic agent. The antitumor efficacy studies in PDX models were performed at Medicilon. Medicilon has established a complete evaluation system for preclinical anti-tumor efficacy, and has more than 200 different types of tumor efficacy models.
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研究人员开发了一种高特异性的CDC7抑制剂TAK-931作为临床肿瘤治疗剂,抗肿瘤药效研究通过永乐高进行
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永乐高进行
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, α1D, and 5-HT2A receptors with Ki<1 nM in a panel of enzyme activity or radioligand binding assays. The binding inhibition activities of MT-1207 were evaluated by Medicilon.
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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永乐高进行
Jul 05,2023
设计、合成和评估具有体内抗炎活性的RIPK1抑制剂,PK研究通过永乐高进行
RIPK1 plays a key role in the necroptosis pathway that regulates inflammatory signaling and cell death in various diseases, including inflammatory and neurodegenerative diseases. Herein, researchers report a series of potent RIPK1 inhibitors, represented by compound 70. Compound 70 possesses favorable pharmacokinetic parameters with moderate clearance and good oral bioavailability in SD rat. The pharmacokinetic parameters were determined at Medicilon using male SD rats (3 rats per group, 4 groups).
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设计、合成和评估具有体内抗炎活性的RIPK1抑制剂,PK研究通过永乐高进行
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