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Jul 11,2023
Chlorpropamide has an anti-aging effect on worms and human lung fibroblast MRC-5 cells. Determination of Chlorpropamide bioavailability in mice was performed by Medicilon
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 mtROS as a pro-longevity signal. Chlorpropamide has an anti-aging effect on worms and human lung fibroblast MRC-5 cells. Determination of Chlorpropamide bioavailability in mice was performed by Medicilon.
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Chlorpropamide has an anti-aging effect on worms and human lung fibroblast MRC-5 cells. Determination of Chlorpropamide bioavailability in mice was performed by Medicilon
Jul 11,2023
BRD4 inhibitors can be used for the treatment of kidney fibrosis. ZLD2218 exhibited the potent inhibitory activity against BRD4. PK analysis of of ZLD2218 were analyzed by Medicilon
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 against BRD4, with the IC50 value of 107 nM. Pharmacokinetic analysis of of ZLD2218 were analyzed by noncompartmental methods using Phoenix WinNonlin 7.0 (Accomplished by Medicilon).
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BRD4 inhibitors can be used for the treatment of kidney fibrosis. ZLD2218 exhibited the potent inhibitory activity against BRD4. PK analysis of of ZLD2218 were analyzed by Medicilon
Jul 11,2023
Immune checkpoint blockade therapies have changed the paradigm of cancer therapies. In vivo studies for anti-PD-1 antibody across 23 syngeneic tumor models were performed by Medicilon
Immune checkpoint blockade therapies have changed the paradigm of cancer therapies. Reseachers performed in vivo screening for anti-PD-1 therapy across 23 syngeneic tumor models and found that CT-26 and Colon 26, which are murine colorectal carcinoma derived from BALB/c mice, showed different sensitivity to anti-PD-1. In vivo studies for anti-PD-1 antibody across 23 syngeneic tumor models were performed by Medicilon.
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Immune checkpoint blockade therapies have changed the paradigm of cancer therapies. In vivo studies for anti-PD-1 antibody across 23 syngeneic tumor models were performed by Medicilon
Jul 11,2023
PDE1 is a promising drug target closely related to central and peripheral diseases
Phosphodiesterase-1 (PDE1) is a promising drug target closely related to central and peripheral diseases. Compound 2j with the IC50 of 21 nM against PDE1B, shows good metabolic stability in the rat liver microsomes. Stability test in the rat liver microsomes were performed by Medicilon.
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PDE1 is a promising drug target closely related to central and peripheral diseases
Jul 11,2023
SKLB-YTH-60 ameliorates inflammation and fibrosis in Bleomycin-induced lung fibrosis mouse models. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon
Idiopathic pulmonary fibrosis is a chronic and lethal lung disease associated with fibroblast activation, myoblast proliferation and extracellular matrix deposition. SKLB-YTH-60 was developed through computer-aided drug design, de novo synthesis and high-throughput screening. YTH-60 has obvious anti‐proliferative activity on fibroblasts and A549 cells. YTH-60 has an acceptable oral bioavailability and appropriate eliminated half-life time. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon.
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SKLB-YTH-60 ameliorates inflammation and fibrosis in Bleomycin-induced lung fibrosis mouse models. The in vivo pharmacokinetic study of YTH‐60 was performed by Medicilon
Jul 11,2023
Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 with orally bioavailable and well tolerated in vivo. PK and MTD assays were performed by Medicilon
PROTAC is an attractive technology in drug discovery. Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 which degrades not only ALK or mutant EGFR but also oncoproteins involved in metastasis. SIAIS164018 is orally bioavailable and well tolerated in vivo. Pharmacokinetic and maximal tolerated dose (MTD) assays were performed by Medicilon.
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Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 with orally bioavailable and well tolerated in vivo. PK and MTD assays were performed by Medicilon
Jul 11,2023
Discovery and preclinical development of orally active and highly selective follicle stimulating hormone receptor agonists. Toxicological evaluations in both rat and dog were performed by Medicilon
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.
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Discovery and preclinical development of orally active and highly selective follicle stimulating hormone receptor agonists. Toxicological evaluations in both rat and dog were performed by Medicilon
Jul 11,2023
PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon
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.
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PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon
Jul 11,2023
Discovery of STAT3 and HDAC dual-pathway inhibitors for the treatment of solid cancer. The PK experiment in SD Rats was carried out by Medicilon
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.
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Discovery of STAT3 and HDAC dual-pathway inhibitors for the treatment of solid cancer. The PK experiment in SD Rats was carried out by Medicilon
Jul 11,2023
Apatinib inhibits Paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway
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).
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Apatinib inhibits Paclitaxel resistance of gastric carcinoma cells through VEGFR2 pathway