产品
编 号：F752777
分子式：C26H28ClF2N7
分子量：512
分子式：C26H28ClF2N7
分子量：512
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CAS No: 2442519-59-5
产品详情
生物活性：
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.
体内研究：
THRX-144644 (2-60 mg/kg; Inhalation: nebulizer, daily, for 14 days) is a Lung-selective inhibitor and targets to the lungs in Sprague Dawley rats.Animal Model:Sprague Dawley rats
Dosage:2, 10, and 60 mg/kg
Administration:Inhalation: nebulizer, daily, for 14 days
Result:Had the L:P ratio (AUC) was 0.44.Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
体外研究：
THRX-144644 (1-10000 nM; 1 h) inhibits ALK5 with an IC50 value of 23 nM in human BEAS2B cell line.
THRX-144644 is a Lung-restricted ALK5 inhibitor with an IC50 value of 0.14 nM. THRX-144644 avoids systemic toxicities associated with TGFβ pathway inhibition.
体内研究：
THRX-144644 (2-60 mg/kg; Inhalation: nebulizer, daily, for 14 days) is a Lung-selective inhibitor and targets to the lungs in Sprague Dawley rats.Animal Model:Sprague Dawley rats
Dosage:2, 10, and 60 mg/kg
Administration:Inhalation: nebulizer, daily, for 14 days
Result:Had the L:P ratio (AUC) was 0.44.Had lung-to-plasma ratios ranged from 100- to 1200-fold in rats across dose level.Had lung trough (24 h) concentrations in rats ranged from 3- to 17-fold above the PCLS IC50 across tolerated doses.
体外研究：
THRX-144644 (1-10000 nM; 1 h) inhibits ALK5 with an IC50 value of 23 nM in human BEAS2B cell line.
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