| Bioactivity | Benzamil (Benzylamiloride), an Amiloride analogue, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM[1][2][3]. |
| Invitro | Benzamil (Benzylamiloride) inhibits neuronal and heterologously expressed small conductance Ca2+-activated K2+ channels[4]. |
| In Vivo | Benzamil (Benzylamiloride) (0.7 mg/kg/day; s.c.) treated stroke-prone spontaneously hypertensive rats (SHRSP) survived, on average, until 16.1 weeks of age in SHRSP rats[5]. |
| Name | Benzamil |
| CAS | 2898-76-2 |
| Formula | C13H14ClN7O |
| Molar Mass | 319.75 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Fischer KG, et al. Characterization of a Na(+)-Ca(2+) exchanger in podocytes. Nephrol Dial Transplant. 2002 Oct;17(10):1742-50. [2]. Wang X, et al. Effects of amiloride, benzamil, and alterations in extracellular Na+ on the rat afferent arteriole and its myogenic response. Am J Physiol Renal Physiol. 2008 Jul;295(1):F272-82. [3]. Dai XQ, et al. Inhibition of TRPP3 channel by amiloride and analogs. Mol Pharmacol. 2007 Dec;72(6):1576-85. [4]. Castañeda MS, et al. Benzamil inhibits neuronal and heterologously expressed small conductance Ca2+-activated K+channels. Neuropharmacology. 2019 Nov 1;158:107738. [5]. Teiwes J, et al. Epithelial sodium channel inhibition in cardiovascular disease. A potential role for amiloride. Am J Hypertens. 2007 Jan;20(1):109-17. |