2387633-15-8
2387633-15-8 structure
- Name: (1-{[2-(3,5-Dichlorophenyl)-6-{[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxy}pyridin-4-yl]methyl}piperidin-4-yl)acetic acid
- Chemical Name: (1-{[2-(3,5-Dichlorophenyl)-6-{[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxy}pyridin-4-yl]methyl}piperidin-4-yl)acetic acid
- CAS Number: 2387633-15-8
- Molecular Formula: C28H32Cl2N6O3
- Molecular Weight: 571.5
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2022-06-26 13:59:18
- Modify Date: 2025-08-26 01:04:00
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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].
| Name | (1-{[2-(3,5-Dichlorophenyl)-6-{[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxy}pyridin-4-yl]methyl}piperidin-4-yl)acetic acid |
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| Description | 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]. |
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| Related Catalog | |
| In Vitro | 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]. Cell Viability Assay[1] Cell Line: CuFi-1 cells Concentration: 17.4 and 263.0 nM Incubation Time: 2 and 48 hours Result: Significantly inhibited ENaC-mediated Na+ transport as measured in differentiated human bronchial epithelial cells under both short- (IC50= 263.0 nM) and long-term (IC50= 17.4 nM) treatment conditions. Cell Viability Assay[1] Cell Line: CuFi-1 cells Concentration: 0.3 μM Incubation Time: 72 hours Result: Significantly increased cell viability in PEA-treated cells to approximately 88% of control levels. Cell Cytotoxicity Assay[1] Cell Line: CuFi-1 cells Concentration: 0.001, 0.01, 0.03, 0.1, 0.3 and 1 μM Incubation Time: 72 hours Result: Provided protection against PEA-mediated cytotoxicity in a dose-dependent manner, over a period of 72 h, with an EC50 of 47.8 nM. |
| References |
| Molecular Formula | C28H32Cl2N6O3 |
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| Molecular Weight | 571.5 |
| Exact Mass | 570.1912943 |