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Submit ReviewBenzamil is a Na+/Ca2+ exhanger (NCX) inhibitor (IC50 ~ 100 nM); TRPP3 channel blocker (IC50 = 1.1 μM for inhibition of Ca2+-activated TRPP3 channel activity). Also non-selective Deg/ENaC family blocker; reduces mechanosensitivity of colonic afferents. More potent derivative of amiloride (Cat. No. 0890).
Benzamil is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 356.21 |
Formula | C13H14ClN7O.HCl |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 161804-20-2 |
PubChem ID | 5702295 |
InChI Key | ZNWMRWWNJBXNKJ-UHFFFAOYSA-N |
Smiles | NC1=C(Cl)N=C(C(NC(NCC2=CC=CC=C2)=N)=O)C(N)=N1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 35.62 | 100 | |
water | 3.56 | 10 |
The following data is based on the product molecular weight 356.21. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.81 mL | 14.04 mL | 28.07 mL |
5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
10 mM | 0.28 mL | 1.4 mL | 2.81 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
References are publications that support the biological activity of the product.
Dai et al (2007) Inhibition of TRPP3 channel by amil. and analogs. Mol.Pharmacol. 72 1576 PMID: 17804601
Fischer et al (2002) Characterization of a Na+-Ca2+ exchanger in podocytes. Nephrol.Dial.Transplant. 17 1742 PMID: 12270979
Page et al (2007) Acid sensing ion channels 2 and 3 are required for inhibition of visceral nociceptors by benzamil. Pain 133 150 PMID: 17467171
If you know of a relevant reference for Benzamil, please let us know.
Keywords: Benzamil, Benzamil supplier, non-selective, Deg, ENaC, family, NCX, sodium, calcium, Na+/Ca2+, exchanger, inhibitors, inhibits, amiloride, derivative, TRPP3, channel, blocker, Exchanger, Epithelial, Sodium, Channels, TRPP, 3380, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Benzamil include:
Singh (2018) Determination of system level alterations in host transcriptome due to Zika virus (ZIKV) Infection in retinal pigment epithelium. Sci Rep 8 11209 PMID: 30046058
Zou et al (2018) Knockout of mitochondrial voltage-dependent anion channel type 3 increases reactive oxygen species (ROS) levels and alters renal sodium transport. J Biol Chem 293 1666 PMID: 29180450
Panja et al (2019) Paraneoplastic cerebellar degeneration: Yo antibody alters mitochondrial calcium buffering capacity. Neuropathol Appl Neurobiol 45 141 PMID: 29679372
Mizuno et al (2019) Development of Orthogonal Linear Separation Analysis (OLSA) to Decompose Drug Effects into Basic Components. Sci Rep 9 1824 PMID: 30755704
Agarwal et al (2017) Transient Opening of the Mitochondrial Permeability Transition Pore Induces Microdomain Calcium Transients in Astrocyte Processes. Neuron 93 587 PMID: 28132831
Do you know of a great paper that uses Benzamil from Tocris? Please let us know.
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Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.