Uncovering new therapeutics for kidney fibrosis hold promise for chronic kidney disease (CKD). BRD4 inhibition ameliorated kidney injury and fibrosis. ZLD2218 exhibited the potent inhibitory activity

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 metho

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

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

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 c

TTK inhibition is an attractive wide-spectrum strategy for cancer therapy. Researchers designed and synthesized a series of pyrido[2, 3-d]pyrimidin-7(8H)-ones as new selective orally bioavailable TTK inhibitors. All the pharmacokinetic studies were carrie

Immune checkpoint inhibition therapies have been used for multiple cancer research. H11-HLE is a tool molecule that allows the interrogation of the contribution of Fc in mediating immune checkpoint therapy. Half-life extended H11 (H11-HLE) induces potent

在馬飛博士帶領(lǐng)下，美迪西經(jīng)驗(yàn)豐富、技術(shù)全面的研究團(tuán)隊(duì)為從Startup到Top 10 Pharma的客戶群提供快捷可靠的Discovery DMPK服務(wù)。服務(wù)領(lǐng)域涵蓋代謝穩(wěn)定性、P450酶抑制、P450酶誘導(dǎo)、酶表型分析、蛋白結(jié)合率、紅細(xì)胞/血漿分配比、Caco-2滲透性、轉(zhuǎn)運(yùn)體研究、代謝產(chǎn)物鑒定、反應(yīng)性代謝產(chǎn)物篩查、各種屬多途徑給藥PK、組織分布與血腦屏障通透性、排泄研究、體內(nèi)藥物相互作用、多周期交叉BE、處方篩選等。

細(xì)胞色素P450構(gòu)成了參與多種內(nèi)源性和外源性化合物代謝的血紅素蛋白的基本家族。CYP1B1能氧化代謝許多前致癌物（如催化多環(huán)芳香烴和芳香胺的活化）和體內(nèi)的甾體激素（如介導(dǎo)17-雌二醇羥化，形成4-兒茶酚雌激素）。