BOS-318 是一种有效的、缓慢解离的、高选择性的、细胞通透性的 Furin 抑制剂，IC50 值为 1.9 nM。BOS-318 可以保护 ENaC 免受中性粒细胞弹性蛋白酶的激活。BOS-318 可用于 CF 肺病的研究。
货号:ajcx38000
CAS:2387633-15-8
分子式:C28H32Cl2N6O3
分子量：571.5
溶解度:DMSO : 50 mg/mL (87.49 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease[1][2].

BOS-318 (0.001-1 μM, 72 hours) provides cytoprotection against toxicity in CuFi-1 cells induced by P aeruginosa exotoxin A (PEA)[1].BOS-318 (U2OS cells) to be approximately 13 times more potent against furin than PCSK5 (IC50 = 25.3 nM), 24 times more potent than PCSK7 (IC50 = 45.8 nM), and 110 times more potent than PCSK6 (IC50 = 209.4 nM) [1].BOS-318 (0.3 μM, 2 hours or 48 hours) reduces ENaC-mediated Na+ absorption in CF HBECs and protects against NE- and CF sputum-sol-mediated activation of the ENaC[1].

[1]. Douglas LEJ, et al. A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease. Cell Chem Biol. 2022 Jun 16;29(6):947-957.e8. [2]. Nayak D, et al. Clearing the air: Uniquely engaging furin as an approach to cystic fibrosis therapy. Cell Chem Biol. 2022 Jun 16;29(6):927-929.