| Bioactivity | 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively[1][2]. | ||||||||||||
| Invitro | 5-(N,N-Hexamethylene)-amiloride inhibits human cardiac ion channels hERG (in CHO cells), Nav1.5 and Cav1.2 (in EHK293 cells) with of 3.3 μM, 30 μM, 8.3 μM, respectively, inelectrophysiology assays[3].5-(N,N-Hexamethylene)-amiloride (1 μM; 0-60 min; 37 ℃) exhibits microsomal stability, (1 μg/mL; 4.2 h; 37 ℃) shows mouse plasma stability and plasma protein binding, (20 μM; 4 h) displays Caco-2 cell permeability, cardiac ion channel activity[3]. Cell Viability Assay[3] Cell Line: | ||||||||||||
| Name | 5-(N,N-Hexamethylene)-amiloride | ||||||||||||
| CAS | 1428-95-1 | ||||||||||||
| Formula | C12H18ClN7O | ||||||||||||
| Molar Mass | 311.77 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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5-(N,N-Hexamethylene)-amiloride
CAS: 1428-95-1 F: C12H18ClN7O W: 311.77
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na+/H+ exchanger inh
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