PLN-1474 (compound 1) 是具有口服活性的，选择性的 avß1 整合素抑制剂，IC₅₀ 值 ＜50 nM。PLN-1474 在肝纤维化小鼠模型中显著降低肝脏 pSMAD3/SMAD3 水平、肝脏胶原蛋白基因表达和肝脏 OHP 浓度。PLN-1474 可用于预防、延缓或治疗纤维化或肝硬化疾病或紊乱的研究。

PLN-1474 (compound 1) is an orally active and selective av?1 integrin inhibitor with an IC 50 value of ＜50 nM. PLN-1474 reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in liver fibrosis mouse model. PLN-1474 can be used for the research of preventing, delaying or treating a fibrotic or cirrhotic disease or disorder.

Solid

IC50: ＜50 nM (ανβ1), ＜50 nM (ανβ6)

PLN-1474 inhibits ανβ1 and ανβ6 with IC50s of ＜50 nM by solid phase assay. has not independently confirmed the accuracy of these methods. They are for reference only.

PLN-1474 (10 μM) decreases the expression level of profibrotic genes, including COL1A1 and TIMP1 in liver.
PLN-1474 significantly reduces levels of pSMAD3/SMAD3 in liver, hepatic collagen gene expression and hepatic OHP concentration in a mouse model of liver fibrosis.
PLN-1474 (6-12 weeks) prophylactically or therapeutically blocks SMAD3 phosphorylation and significantly decreases OHP levels, collagen gene expression, and collagen deposition examined histologically in the CDAHFD NASH mouse model. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Anderson Kraig, et al. Combination treatment of liver diseases using integrin inhibitors. WO2021127483. 2021.

In Vitro: DMSO : ≥ 83.33 mg/mL (193.09 mM)配制储备液