| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
CA Ⅱ
Carbonic anhydrase I (Ki 15 nM), Carbonic anhydrase II (Ki 9 nM), Carbonic anhydrase III (CAS3, Ki 54 nM), also inhibits low-threshold calcium currents. |
|---|---|
| ln Vitro |
Benzolamide inhibits hCA I, hCA II, EcoCAγ, and VchCAγ with corresponding Ki values of 15 nM, 9 nM, 94 nM, and 78 nM [1]. Whereas CAS1 (Ki=2115 nM) and CAS2 (Ki= 410 nm) are less selective than CAS3 (Ki=54 nM) when it comes to benzonzoamide [2].
In vitro, Benzolamide is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM for hCA I, 9 nM for hCA II, 94 nM for EcoCAy, and 78 nM for VchCAy. It also inhibits CAS3 (carbonic anhydrase III) with a Ki of 54 nM. It inhibits low-threshold calcium currents in hippocampal pyramidal neurons. It is used as a research tool for studying CA function in glaucoma, epilepsy, and neuronal excitability. |
| ln Vivo |
Rats treated with benzolamide (90 μmol/kg; intraperitoneally) have lower brain pH and fewer electroencephalographic post-asphyxia epileptic episodes[3].
In vivo, Benzolamide is used in research for glaucoma and epilepsy. It reduces intraocular pressure (IOP) by inhibiting CA in the ciliary body. It has also been studied for its anticonvulsant effects. No specific detailed in vivo data is provided in the search results, but it is a known CA inhibitor with in vivo efficacy in animal models of glaucoma and seizures. |
| Enzyme Assay |
Recombinant human carbonic anhydrase isozymes (hCA I, hCA II) are expressed in E. coli and purified. The CA activity assay measures the esterase activity of CA using 4-nitrophenyl acetate (NPA) as substrate, or the CO2 hydration activity using a stopped-flow pH indicator method. For NPA: reaction contains Tris-SO4 buffer (pH 7.4), NPA (0.8 mM), and varying concentrations of Benzolamide (0.1-1000 nM). The change in absorbance at 348 nm is monitored for 5-10 minutes. Ki values are determined from dose-response curves (15 nM for hCA I, 9 nM for hCA II). For CAS3, a separate assay is performed, yielding a Ki of 54 nM.
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| Cell Assay |
For calcium current inhibition, rat hippocampal pyramidal neurons are isolated and cultured. Whole-cell patch-clamp recordings are performed. Low-threshold calcium currents are activated by depolarizing steps from a holding potential of -90 mV to -40 mV. Benzolamide (10-500 uM) is applied, and the inhibition of calcium current is measured. For CA inhibition in cells, primary choroid plexus epithelial cells or ciliary body cells expressing CA can be used. Cells are treated with Benzolamide (0.1-100 uM), and cellular CA activity is measured by CO2 hydration assay in lysates.
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| Animal Protocol |
Animal/Disease Models: Male and female Wistar Han rats (11-day-old)[3]
Doses: 90 µmol/kg Route of Administration: A single ip Experimental Results: Induced a fast brain acidosis of a comparable magnitude. Suppressed electrographic seizures after asphyxia by slowing down the recovery of brain pH. For IOP reduction, New Zealand white rabbits with experimentally induced glaucoma are used. Benzolamide is formulated in a suitable vehicle and administered orally or intravenously. IOP is measured using a tonometer at multiple time points post-dose. For anticonvulsant activity, the maximal electroshock seizure (MES) test in mice is used: mice are administered Benzolamide (10-100 mg/kg, i.p.), and protection against hindlimb tonic extension is measured. ED50 values can be calculated. |
| ADME/Pharmacokinetics |
No specific PK data for Benzolamide provided in the search results. Benzolamide is a sulfonamide CA inhibitor. Its PK properties are likely similar to other CA inhibitors: oral bioavailability (variable), moderate half-life (2-5 hours), and protein binding (high). It is excreted in urine. The compound is known to have poor CNS penetration compared to acetazolamide.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Benzolamide in the search results. As a carbonic anhydrase inhibitor, the primary on-target toxicity is metabolic acidosis. Other side effects include paresthesia (tingling in the extremities), altered taste, diuresis, and fatigue. Sulfonamides can cause allergic reactions (rash, fever, Stevens-Johnson syndrome). For research use, handle with standard precautions.
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| References |
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| Additional Infomation |
Selective renal carbonic anhydrase inhibitor. It may also be used to treat certain cases of respiratory failure.
Benzolamide (CL11366, CAS: 3368-13-6) is a potent carbonic anhydrase inhibitor used as a research tool for studying glaucoma, epilepsy, and CA function. It is also known as CL-11366. It is not approved for clinical use in most countries, though it has been studied as a diuretic and antiglaucoma agent. Molecular formula: C8H8N4O4S3, MW 320.36. For research use only. References: Maren TH. (1976). |
| Molecular Formula |
C8H8N4O4S3
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|---|---|
| Molecular Weight |
320.37
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| Exact Mass |
319.971
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| CAS # |
3368-13-6
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| PubChem CID |
18794
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| Appearance |
White to light yellow solid powder
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| Density |
1.746g/cm3
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| Boiling Point |
585.9ºC at 760mmHg
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| Flash Point |
308.2ºC
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| Index of Refraction |
1.689
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| LogP |
2.921
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
503
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)S(=O)(=O)NC2=NN=C(S2)S(=O)(=O)N
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| InChi Key |
PWDGTQXZLNDOKS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H8N4O4S3/c9-18(13,14)8-11-10-7(17-8)12-19(15,16)6-4-2-1-3-5-6/h1-5H,(H,10,12)(H2,9,13,14)
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| Chemical Name |
5-(benzenesulfonamido)-1,3,4-thiadiazole-2-sulfonamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (780.35 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.49 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1214 mL | 15.6070 mL | 31.2139 mL | |
| 5 mM | 0.6243 mL | 3.1214 mL | 6.2428 mL | |
| 10 mM | 0.3121 mL | 1.5607 mL | 3.1214 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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