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Jul 11,2023
H11-HLE is a tool molecule that allows the interrogation of the contribution of Fc in mediating immune checkpoint therapy with potent anti-tumor efficacy
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 anti-tumor efficacy in mouse syngeneic tumor models. Authors gratefully acknowledge performing in vivo studies by Medicilon Preclinical Research LLC who performed the in vivo experiments.
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H11-HLE is a tool molecule that allows the interrogation of the contribution of Fc in mediating immune checkpoint therapy with potent anti-tumor efficacy
Jul 11,2023
JND003 is a selective ERRα agonist alleviating nonalcoholic fatty liver disease and insulin resistance. Pharmacokinetics and tissue distribution assays were performed at Medicilon
Nonalcoholic fatty liver disease (NAFLD) is one of the most prevalent forms of chronic liver diseases. Estrogen-related receptor alpha (ERRα) is a viable target for NAFLD. JND003 is a potent and selective ERRα agonist alleviating nonalcoholic fatty liver disease and insulin resistance. JND003 is orally bioavailable and exhibits high grade of distribution in liver and abdominal adipose tissues. Pharmacokinetics (PK) and Tissue Distribution Assays of JND003 were performed at Medicilon.
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JND003 is a selective ERRα agonist alleviating nonalcoholic fatty liver disease and insulin resistance. Pharmacokinetics and tissue distribution assays were performed at Medicilon
Jul 11,2023
Discovery of novel PDE4 inhibitors for the topical treatment of Psoriasis. The metabolic stability on mouse, rat, and human liver microsomes was determined by Medicilon
Psoriasis is a common immune-mediated skin disorder manifesting in abnormal skin plaques, and PDE4 is an effective target for the treatment of inflammatory diseases such as psoriasis. Researchers designed and synthesized the lead compound with high PDE4 inhibitory potency and remarkable metabolite profiles in liver microsomes. The metabolic stability on mouse, rat, and human liver microsomes was determined by Medicilon.
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Discovery of novel PDE4 inhibitors for the topical treatment of Psoriasis. The metabolic stability on mouse, rat, and human liver microsomes was determined by Medicilon
Jul 11,2023
Synthesis of selective PAK4 inhibitors for lung metastasis of lung cancer and melanoma cells. The pharmacokinetic study of the selective PAK4 inhibitor was carried out by Medicilon
The p21 activated kinase 4 (PAK4) is serine/threonine protein kinase that is critical for cancer progression. 6-Ethynyl-1H-indole derivative 55 is a potent and selective PAK4 inhibitor (Ki=10.2 nM). Compound 55 is effective in the treatment of metastatic cancer. The pharmacokinetic study of Compound 55 was carried out by Medicilon.
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Synthesis of selective PAK4 inhibitors for lung metastasis of lung cancer and melanoma cells. The pharmacokinetic study of the selective PAK4 inhibitor was carried out by Medicilon
Jul 11,2023
Targeted protein degradation exemplified by PROTACs is an emerging strategy for drug discovery
Targeted protein degradation (TPD) exemplified by PROTACs is an emerging strategy for next generation drug discovery. Threonine tyrosine kinase (TTK) is a dual-specific protein kinase that catalyzes phosphorylation of both serine/threonine and tyrosine residues. Researchers designed and synthesized TTK PROTACs, which demonstrated reasonable pharmacokinetic profiles. All the pharmacokinetic studies were carried out by Medicilon, according to the protocols and guidelines of the institutional care and use committee.
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Targeted protein degradation exemplified by PROTACs is an emerging strategy for drug discovery
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