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CWHM-12

CAS No. : 1564286-55-0

MCE 站：CWHM-12

产品活性：CWHM-12是αV整联蛋白的有效抑制剂，抑制αvβ8，αvβ3，αvβ6和αvβ1的 IC₅₀ 值分别为0.2，0.8，1.5，1.8 nM。

研究领域：Cytoskeleton

作用靶点：Integrin

In Vitro: CWHM-12 (CWHM 12) also less potently inhibits αvβ5 (IC₅₀=61 nM) and αIIbβ3/α2β1/α10β1 (IC₅₀>5000 nM). CWHM-12 demonstrates high potency against all of the five possible β subunit binding partners (αvβ1, αvβ3, αvβ5, αvβ6 and αvβ8) in in vitro ligand-binding assays, with somewhat less potency against αvβ5 than against the other αv integrins.

In Vivo: Mice are treated with CCl₄ for 3 weeks to establish fibrotic disease and then treated with CWHM-12 (CWHM 12) or vehicle for the final 3 weeks of CCl₄. CWHM-12 significantly reduces liver fibrosis even after fibrotic disease have been established. Digital image quantitation demonstrates significantly reduced p-SMAD3 signaling in the livers of CWHM-12 treated mice compare to controls, demonstrating that the protection from CCl₄-induced hepatic fibrosis observed in CWHM-12 treated mice is due at least in part to a reduction in TGF-β activation by αv integrins. Besides, administration of CWHM-12 significantly inhibited progression of pulmonary fibrosis.

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