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Oct 21,2025
5年3项顺应症!yl23455永利助力泰恩康CKBA乳膏再获临床试验批准
作为泰恩康的恒久相助同伴,,yl23455永利依托临床前研发效劳平台,,为CKBA乳膏提供了小型猪药代动力学研究、制剂清静性评价、体内光毒性试验等研究效劳。。
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5年3项顺应症!yl23455永利助力泰恩康CKBA乳膏再获临床试验批准
Oct 17,2025
高效环保:Medicilon助力乐成合成高性能海洋抗污化合物Butenolide
Biofouling is one of the most serious problems in the maritime industry and aquaculture development. In the marine environment, submerged surfaces are often colonized by marine organisms that have come to be called biofoulers, which are marine organisms that attach to submerged surfaces. Biofoulers increase the weight, drag and surface corrosion of ships, and lead to huge costs to maintain mariculture systems and seawater pipelines. Antifouling compounds are used as biocides in marine paints that are coated on the submerged surfaces to control the preponderance of biofoulers. Butenolide [5-octylfuran-2(5H)-one] is a very promising anti-marine-fouling compound. The antifouling compound 5-octylfuran-2(5H)-one (here referred to as butenolide) was synthesized by Medicilon.
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高效环保:Medicilon助力乐成合成高性能海洋抗污化合物Butenolide
Oct 16,2025
靶向PXR:自然产品衍生物调控药物代谢新战略!本研究中卵白表达与纯化通过yl23455永利举行
Nuclear receptors are ligand-activated transcription factors involved in regulating many physiologic and pathologic processes. Ligand binding to nuclear receptors leads to dissociation of co-repressors, recruitment of co-activators, and subsequent activation of gene expression. Because of their associations with many human diseases, nuclear receptors are therapeutic targets for pharmaceutical development. The pregnane X receptor (PXR, NR1I2) belongs to the nuclear receptor family. The activity of PXR can be controlled by the binding of small molecule agonists or antagonists. Because of its unique ligand binding pocket, PXR binds promiscuously to structurally diverse chemicals. PXR regulates the expression of proteins such as drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4), efflux transporter P-glycoprotein, and other multidrug resistance proteins, which are involved in metabolism and elimination of potentially harmful chemicals. PXR has been detected in various tissues including kidney, colon, brain capillaries, small intestine, and predominantly in liver, and it can be activated by various ligands that bind to its ligand binding domain (LBD). PXR forms a heterodimeric complex with RXR to activate gene transcription. The recombinant pETDuet1-hPXR-LBD/mSRC-1 plasmid (Medicilon, Shanghai, China) was transformed into Escherichia coli BL21 DE3 cells for protein expression.
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靶向PXR:自然产品衍生物调控药物代谢新战略!本研究中卵白表达与纯化通过yl23455永利举行
Oct 16,2025
抗癌新希望:强效Smac模拟物SM-1200引发长期肿瘤消退,,极具临床潜力!本研究中PK实验通过yl23455永利举行
SM-1200, a potent bivalent Smac mimetic, induces rapid, complete, and durable tumor regression in mice. X-linked inhibitor of apoptosis protein (XIAP) and cellular IAP1/2 (cIAP1/2) regulate apoptosis and are promising cancer therapeutic targets. Smac (second mitochondria-derived activator of caspases), also known as DIABLO, antagonizes IAP proteins. Researchers designed and synthesized new compounds based on bivalent Smac mimetics, leading to the identification of SM-1200 (compound 12). SM-1200 binds to XIAP (Ki = 0.5 nM), cIAP1 (Ki = 3.7 nM), and cIAP2 (Ki = 5.4 nM), and inhibits growth of MDA-MB-231 breast cancer (IC50 = 11.0 nM) and SK-OV-3 ovarian cancer (IC50 = 28.2 nM) cell lines. With an improved pharmacokinetic profile compared to previous bivalent Smac mimetics, SM-1200 effectively induces rapid and durable tumor regression in the MDA-MB-231 xenograft model. These findings suggest SM-1200 is a promising Smac mimetic and warrants extensive evaluation as a potential candidate for clinical development. Pharmacokinetic (PK) studies of bivalent Smac mimetics were performed in male Sprague Dawley rats (body weight: 250–270 g) by Medicilon. Before the pharmacokinetic studies, animals were carotid cannulated.
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抗癌新希望:强效Smac模拟物SM-1200引发长期肿瘤消退,,极具临床潜力!本研究中PK实验通过yl23455永利举行
Oct 15,2025
卓越成药性:高效AR-PROTAC降解剂ARD-2051在多个物种中展现优质PK属性与口服生物使用度!本研究中PK实验通过yl23455永利举行
Prostate cancer (PCa) is a major global health concern. The androgen receptor (AR), a key member of the nuclear hormone receptor superfamily, is vital for prostate gland development and the maintenance of male secondary sexual characteristics. ARD-2051 is a potent and orally bioavailable AR PROTAC degrader. In vitro microsomal metabolic stability studies of AR degraders were performed in Medicilon. The in vitro plasma stability of a test compound was studied in human, mouse, rat, dog and monkey plasmas in Medicilon. Plasma protein binding of a test compound was assessed by equilibrium dialysis method with dialysis membrane strips in Medicilon. The CYP inhibition of a test compound was studied in human liver microsomes in Medicilon. PK studies in mice, rats and dogs were performed in Medicilon. In mouse, ARD-2051 has an excellent overall PK profile, with a low clearance (Cl = 3.7 ml/min/kg), a moderate volume of distribution (Vss = 1.3 L/kg), a half-life of approximately 5 h with both IV and oral routes of administration, and an excellent oral exposure with a good oral bioavailability (F) of 53%. In rat, ARD-2051 has a low-moderate clearance in rats (Cl = 10.2 ml/min/kg), a moderate volume of distribution (Vss = 1.3 L/kg), a half-life of 2-2.3 h with intravenous (IV) and oral routes of administration, and achieves an excellent oral bioavailability (F) of 82%. In dog, ARD-2051 has a low-moderate clearance (Cl = 4.6 ml/min/kg), a good volume of distribution (Vss = 2.8 L/kg), a long half-life of 8.9 h with IV route of administration and 21.1 h with oral route of administration, an excellent oral exposure (Cmax = 294 ng/ml and AUC=1822 h*mg/ml at 1 mg/kg), and an oral bioavailability (F) of 46%. These data indicate that ARD-2051 has favorable pharmacokinetic properties and excellent oral bioavailability in mice, rats, and dogs.
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卓越成药性:高效AR-PROTAC降解剂ARD-2051在多个物种中展现优质PK属性与口服生物使用度!本研究中PK实验通过yl23455永利举行
Oct 15,2025
剂型刷新:果冻制剂提升药物吸收,,改善用药依从性!本研究中PK实验通过yl23455永利举行
Jellies offer a palatable alternative to traditional tablets, improving medication adherence in children and the elderly. A study comparing different formulations of common cold medicines (syrup, jellies, and tablets) revealed that while none were bioequivalent according to FDA standards, jellies and syrup exhibited similar absorption rates and extents. Tablets, however, significantly delayed and reduced drug absorption compared to the syrup. These findings suggest that jellies can be a patient-friendly formulation with comparable bioavailability to syrup. To evaluate the effect of jelly formulation on the bioavailability of cold medicines, two types of jellies were prepared for a fixed-dose combination of acetaminophen (AAP), chlorpheniramine maleate (CPM), dextromethorphan hydrobromide (DMH), and dl-methylephedrine hydrochloride (MEH). A pharmacokinetic study was performed in beagle dogs after oral administration in Medicilon Preclinical Research (Shanghai) LLC (Shanghai, China). The plasma concentration profiles of AAP, CPM, DMH, and MEH are presented in the figure below. As shown in the initial plasma concentration profile for 4 h, the jellies and syrup showed rapid absorption of AAP, while both tablets retarded the absorption of AAP exhibiting lower Cmax and delayed Tmax. The jellies had less delay in the absorption rate and better bioavailability than the tablets.
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剂型刷新:果冻制剂提升药物吸收,,改善用药依从性!本研究中PK实验通过yl23455永利举行
Oct 11,2025
yl23455永利助力战略相助同伴SAPU Sapu003在澳大利亚获得临床试验批准
作为SAPU的战略相助同伴,,yl23455永利依附一站式生物医药临床前研发效劳平台,,为Sapu003提供了CMC放行验证(正在举行中)、药代动力学、清静性评价以及IND申报等无缝衔接、高效联动的临床前研发效劳,,为其IND申报按下加速键。。
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yl23455永利助力战略相助同伴SAPU Sapu003在澳大利亚获得临床试验批准
Sep 18,2025
yl23455永利助力相助同伴济民可信中药1.2类新药JMZ-2102和JMZ-2102胶囊获批临床
yl23455永利作为济民可信的恒久相助同伴,,为JMZ-2102和JMZ-2102胶囊提供了从顺应症设计、活性因素筛选到系统药效学评价的效劳。。?双方协同互补,,为该药物的高效推进和乐成获批临床提供了要害支持。。
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yl23455永利助力相助同伴济民可信中药1.2类新药JMZ-2102和JMZ-2102胶囊获批临床
Sep 18,2025
非阿片类镇痛新药破局!yl23455永利助力艾立康药业外周镇痛药物获批临床
作为艾立康药业的相助同伴,,yl23455永利依附扎实的药效评价能力和高质量的效劳,,为ALK2401片提供了临床前药效学研究支持,,有力加速了该药物的研发历程。。
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非阿片类镇痛新药破局!yl23455永利助力艾立康药业外周镇痛药物获批临床
Sep 04,2025
破局痛风药物清静逆境!yl23455永利助力横琴新创益F-02-2-Na中美双报双批
yl23455永利作为横琴新创益的战略相助同伴,,为F-02-2-Na提供了切合中美双报标准的药效试验效劳,,助力其快速获批临床。。
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破局痛风药物清静逆境!yl23455永利助力横琴新创益F-02-2-Na中美双报双批
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