Bexotegrast,2376257-44-0

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Bexotegrast

CAS No. : 2376257-44-0

MCE 国际站：Bexotegrast

产品活性：Bexotegrast (PLN-74809) 是一种具有口服活性的，有效的双重 αvβ6/αvβ1 整合素抑制剂，K_d 分别为 5.7 nM 和 3.4 nM。Bexotegrast 抑制 αvβ6 和 αvβ1 诱导的 TGF-β 激活，IC₅₀ 值分别为 29.8 nM 和 19.2 nM。Bexotegrast 具有抗纤维化作用，可阻断纤维化肺中 TGF-β 激活的多种途径。

研究领域：Cytoskeleton

作用靶点：Integrin

In Vitro: Bexotegrast (PLN-74809; 1.82 µM; 7-day incubation) significantly reduces collagen type I alpha I (COL1A1) mRNA expression by 54% in precision-cut lung slices (PCLSs). PLN-74809 shows an approximately 50% reduction in Smad2 phosphorylation.
Bexotegrast (1.82 µM; 3-day incubation) dose-dependently reduces Col1a1 mRNA expression in PCLSs prepared from fibrotic mouse lungs by up to 71%.
Bexotegrast fully inhibits αvβ6 integrin-mediated adhesion to LAP by normal human bronchial epithelial cells with an IC₅₀ of 39.3 nM.

In Vivo: Bexotegrast (PLN-74809; orally; 100, 250, and 500 mg/kg twice daily; from Day 7 to Day 21) shows a dose-dependent, significant reduction in interstitial fibrillar collagen deposition in Bleomycin-challenged mice. Bexotegrast dose-dependently blocks Smad3 phosphorylation.

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