Jul 06,2023

開(kāi)發(fā)具有口服活性的高度選擇性卵泡刺激激素受體激動(dòng)劑，且進(jìn)行臨床前研究。其中對(duì)大鼠和狗的毒理學(xué)評(píng)估通過(guò)尊龍凱時(shí)進(jìn)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 methods or in high complexity methods. TOP5300 was evaluated in standard ADME, including Cytochrome P450 inhibition, clearance and pharmacokinetic profiles. Toxicological evaluations were performed in both rat and dog as the second species according to the guidance from FDA. These assays were performed by Medicilon.

Jul 06,2023

PARP1/2抑制劑有治療腫瘤的潛力，PARP1/2抑制實(shí)驗(yàn)通過(guò)尊龍凱時(shí)進(jìn)行

Poly ADP-ribose polymerases (PARPs) are a family of enzymes related to DNA damage repair process. Inhibition of PARP1/2 accelerates the damage of injured DNA, which is synthetically lethal to DNA-repairing-deficient cancer cells, such as BRCA1/2-deficient cells. PARP1/2 inhibitors could be a promising candidate for the treatment of cancer. The PARP1 and PARP2 inhibition assays were performed by Medicilon.

Jul 06,2023

使用尊龍凱時(shí)硒代氨基酸培養(yǎng)基產(chǎn)品發(fā)表的學(xué)術(shù)文獻(xiàn)

尊龍凱時(shí)提供全套M9硒代蛋氨酸（SeMET）培養(yǎng)基，可用于IPTG誘導(dǎo)的大腸桿菌表達(dá)系統(tǒng)，生產(chǎn)硒代蛋氨酸標(biāo)記的蛋白，運(yùn)用多波長(zhǎng)反常散射（MAD）方法進(jìn)行蛋白質(zhì)晶體學(xué)研究。

Jul 05,2023

設(shè)計(jì)合成一種高度選擇性的H435R突變敏感的甲狀腺激素受體β激動(dòng)劑，PK分析通過(guò)尊龍凱時(shí)進(jìn)行

Thyroid hormone receptors (TRs) are ligand-dependent transcription factors that belong to the nuclear receptor superfamily and also participate in important physiological functions. In this study, Compound 16g is a well-characterized selective and mutation-sensitive TRβ agonist for further investigating its function in treating dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH). Compound 16g showed excellent lipid metabolism, safety, metabolic stability, and pharmacokinetic properties. PK properties of Compound 16g were analyzed by Medicilon.

Jul 05,2023

研究人員設(shè)計(jì)合成STAT3和HDAC雙通路抑制劑用于治療實(shí)體腫瘤，PK實(shí)驗(yàn)通過(guò)尊龍凱時(shí)進(jìn)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 HDAC inhibitors in solid tumors. Herein, researchers synthesized a series of potent pterostilbene hydroxamic acid derivatives with dual-target inhibition activity. The pharmacokinetic experiment in SD Rats was carried out by Medicilon.

Jul 05,2023

阿帕替尼通過(guò)VEGFR2通路抑制紫杉醇對(duì)胃癌細(xì)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 signaling pathway. In this research, the VEGFR2 sequences were designed and then amplified by RT-PCR. The sequences were then ligated with a pcDNA3.0 plasmid to construct a recombinant pcDNA3.0-VEGFR2 vector (Medicilon).

Jul 05,2023

研究人員報(bào)告了一種具有細(xì)胞滲透性的選擇性METTL3納摩爾抑制劑UZH1a，作者感謝尊龍凱時(shí)合成了UZH1a和UZH1b

The methylase METTL3 is the writer enzyme of the N6‐methyladenosine (m6A) modification of RNA. Here researchers report a nanomolar inhibitor of METTL3 (UZH1a) which is selective and cell‐permeable, while its enantiomer UZH1b is essentially inactive. The authors thank Medicilon for the synthesis of the UZH1a and UZH1b compounds.

Jul 05,2023

研究人員設(shè)計(jì)并合成了一種光籠PI3K抑制劑1，它可以通過(guò)紫外線照射激活，釋放出高效PI3K抑制劑2。化合物1和2的ADME研究通過(guò)尊龍凱時(shí)進(jìn)行

Aberrant activation of the PI3K pathway has been intensively targeted for cancer therapeutics for decades. In this work, researchers designed and synthesized a novel photocaged PI3K inhibitor 1, which could be readily activated by UV irradiation to release a highly potent PI3K inhibitor 2. ADME studies of compounds 1 and 2 were conducted by Medicilon. Medicilon's pharmacokinetics department offers the clients a broad spectrum of high quality of services in the areas of in vitro ADME, in vivo pharmacokinetics and bioanalysis services, ranging from small molecules to large molecules, such as protein and antibody.

Jul 05,2023

RIPK2激酶參與多種慢性炎癥，UH15-15抑制RIPK2激酶并具有良好的體外ADME和PK特性，PK研究通過(guò)尊龍凱時(shí)進(jìn)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 chronic inflammatory conditions. UH15-15 inhibits RIPK2 kinase (IC50=8 nM) and demonstrates favorable in vitro ADME and pharmacokinetic properties. The pharmacokinetic study was conducted by Medicilon.

Jul 05,2023

合成具有體內(nèi)抗腫瘤活性的強(qiáng)效PD-L1抑制劑，并進(jìn)行生物學(xué)評(píng)價(jià)和機(jī)制研究。PK研究通過(guò)尊龍凱時(shí)進(jìn)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.