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编 号：F756981
分子式：C22H22N4O
分子量：358.44
分子式：C22H22N4O
分子量：358.44
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CAS No: 2925744-43-8
产品详情
生物活性：
CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages.
体内研究：
CSF1R-IN-15 体内药代动力学指标来自于盒式给药研究。CSF1R-IN-15 在 C57BLKS 小鼠中的 t1/2，C0，AUC0-∞，CLobs 和 Vss,obs 分别为 0.5 h，37 ng/ml，18 h*ng/ml，54 L/h/kg 和 32 L/k。Animal Model:In Vivo Pharmacokinetic Study
Dosage:1mg/kg
Administration:Intravenous injection (i.v.) single dosing of drugs (1 mg/kg each) in a 20% DMSO, 80% PEG400 formulation. Blood sampling was done after 10, 30, 60, 120, 240, and 480 min.
Result:In vivo pharmacokinetic indexes were t1/2 (0.5 h), C0 (37 ng/mL), AUC0-∞ (18 h*ng/mL), CLobs (54 L/h/kg), and Vss,obs (32 L/kg), respectively.
体外研究：
CSF1R-IN-15 (0.007-10 μM, 72 h) 对 Ba/F3 细胞没有活性，而 pexidartinib (HY-16749) 具有优越的活性。CSF1R-IN-15 对血浆蛋白结合的评估是通过平衡透析法进行的。CSF1R-IN-15 (5 μM, 6 h, 37 °C) 与血浆孵化，与小鼠血浆蛋白结合率为 69%。
CSF1R-IN-15 (compound 23) is an inhibitor targeting CSF1R. The colony-stimulating factor-1 receptor (CSF1R) is a tyrosine kinase embedded in the cell membrane of macrophages. The receptor is activated by colony-stimulating factor-1 (CSF-1) and interleukin-34, and signaling via CSF1R is crucial for the differentiation, proliferation, and survival of macrophages.
体内研究：
CSF1R-IN-15 体内药代动力学指标来自于盒式给药研究。CSF1R-IN-15 在 C57BLKS 小鼠中的 t1/2，C0，AUC0-∞，CLobs 和 Vss,obs 分别为 0.5 h，37 ng/ml，18 h*ng/ml，54 L/h/kg 和 32 L/k。Animal Model:In Vivo Pharmacokinetic Study
Dosage:1mg/kg
Administration:Intravenous injection (i.v.) single dosing of drugs (1 mg/kg each) in a 20% DMSO, 80% PEG400 formulation. Blood sampling was done after 10, 30, 60, 120, 240, and 480 min.
Result:In vivo pharmacokinetic indexes were t1/2 (0.5 h), C0 (37 ng/mL), AUC0-∞ (18 h*ng/mL), CLobs (54 L/h/kg), and Vss,obs (32 L/kg), respectively.
体外研究：
CSF1R-IN-15 (0.007-10 μM, 72 h) 对 Ba/F3 细胞没有活性，而 pexidartinib (HY-16749) 具有优越的活性。CSF1R-IN-15 对血浆蛋白结合的评估是通过平衡透析法进行的。CSF1R-IN-15 (5 μM, 6 h, 37 °C) 与血浆孵化，与小鼠血浆蛋白结合率为 69%。
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