Benzamil

Benzamil

Benzamil amiloride
An Inhibitor of Na⁺/Ca²⁺ Exchangers and a Blocker of ASIC, TRPP3 and TRPA1 Channels
Cat #: B-161
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
Source: Synthetic
MW: 319.75 Da.
Target: Na⁺/Ca²⁺ exchangers, ASIC/ENaC, TRPP3, TRPA1 channels
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Benzamil is a potent amiloride analogue that acts as an inhibitor of Na⁺/Ca²⁺ exchangers and a blocker of ASIC/DEG/ENaC, TRPP3, and TRPA1 channels displaying IC₅₀ of 0.1, 1.1 and 55 µM respectively^1-3.

Benzamil is commercially available as an inhibitor for acid sensing ion channels (ASICs) belonging to Deg/ENaC family. The compound is also well known as a diuretic compound that is used for the management of congestive heart disease or hypertension. Intrathecal administration of benzamil demonstrates antinocicepitve effects in several pain models in animals and humans through the inhibition of acid sensing ion channels⁴.

Alomone Labs is pleased to offer Benzamil (#B-161).

References

1. Fischer, K.G. et al. (2002) Nephrol. Dial. Transplant 17, 1742.
2. Dai, X.Q. et al. (2007) Mol. Pharmacol. 72, 1576.
3. Banke, T.G. (2011) Brain Res. 1381, 21.
4. Jeong. S. et al. (2013) J. Korean Med. Sci. 28, 1238.

• Our Bioassay
• Specifications
• Related Products

Our bioassay

Alomone Labs Benzamil inhibits ASIC3 channels expressed in Xenopus oocytes.

A. Time course of Benzamil (#B-161) inhibition of ASIC3 channels current. Membrane potential was held at -60 mV, current was elicited every 50 sec by transient applications of pH 5.5, and was inhibited significantly by a 4 min application of 50 µM Benzamil (horizontal bar). B. Superimposed traces of ASIC3 currents upon application of control and of 50 µM Benzamil, as indicated, taken from the experiment in A.

Alomone Labs Benzamil inhibits TRPA1 currents induced by AITC in HEK-293 cells.
Dose response curve of Benzamil (#B-161) inhibition of human TRPA1-mediated increase in intracellular Ca²⁺. Cells were loaded with Calcium 5 dye, incubated with Benzamil, and stimulated with 1 µM allyl isothiocyanate (EC₈₀). Changes in intracellular Ca²⁺ following stimulation were detected as changes in relative fluorescence (RFU).
Purity>99%.
Effective concentration1-300 µM.
Chemical name3,5-diamino-N-(N'-benzylcarbamimidoyl)-6-chloropyrazine-2-carboxamide.
Molecular formulaC₁₃H₁₄ClN₇O.
CAS number161804-20-2.
ActivityBenzamil is a potent amiloride analogue, an inhibitor of the Na⁺/Ca²⁺exchanger (IC₅₀ = 0.1 µM) ¹, a blocker of Deg/ENaC channels ², of TRPP3 channels (IC₅₀ = 1.1 µM) ³ and of TRPA1 channels (IC₅₀ = 55 µM)⁴.
Storage before reconstitutionStore at +4^oC.
Reconstitution

Up to 100 mM in DMSO.
Centrifuge all products before use (10000 x g 5 min).

Storage after reconstitutionUp to three months at -20°C.