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Benzolamide

CAS No.: 3368-13-6

Benzolamide (CL 11366) inhibits carbonic anhydrase effectively and low-threshold calcium currents in hippocampal pyramid
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Description Benzolamide (CL 11366) inhibits carbonic anhydrase effectively and low-threshold calcium currents in hippocampal pyramidal neurons.
In vitro Benzolamide inhibits hCA I, hCA II, EcoCAγ and VchCAγ, with Kis of 15 nM, 9 nM, 94 nM and 78 nM, respectively[1]. Benzolamide shows selectivity for CAS3 with a Ki of 54 nM over CAS1 with a Ki of 2115 nM and CAS2 with a Ki of 410 nM[2].
In vivo 给予大鼠90 μmol/kg的Benzolamide能够降低脑部pH值,并抑制缺氧后电图发作[3]。
Target activity CA (human):15 nM (Ki), VchCAγ:78 nM (Ki), CA II (human):9 nM (Ki), CAS3:54 nM (Ki), EcoCAγ:94 nM (Ki)
Synonyms CL-11366, W 1803, CL 11366, CL11366, 苯唑拉胺, W-1803
molecular weight 320.37
Molecular formula C8H8N4O4S3
CAS 3368-13-6
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: 250 mg/mL (780.35 mM), Sonication is recommended.
References 1. Prete SD, et, al. Escherichia coli γ-carbonic anhydrase: characterisation and effects of simple aromatic/heterocyclic sulphonamide inhibitors. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1545-1554. 2. Vullo D, et, al. Sulfonamide Inhibition Studies of the β-Class Carbonic Anhydrase CAS3 from the Filamentous Ascomycete Sordaria macrospora. Molecules. 2020 Feb 25;25(5):1036. 3. Pospelov AS, et, al. Carbonic anhydrase inhibitors suppress seizures in a rat model of birth asphyxia. Epilepsia. 2021 Jun 27. 4. Cecchi A, Winum JY, Innocenti A, Vullo D, Montero JL, Scozzafava A, Supuran CT. Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/tumor-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides derived from 4-isothiocyanato-benzolamide. Bioorg Med Chem Lett. 2004 Dec 6;14(23):5775-80. PubMed PMID: 15501039.