[CAS NO. 3368-13-6] Benzolamide
PRODUCTS SPECIFICATIONS [3368-13-6]
DESCRIPTION [3368-13-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 320.37 |
| Molecular Formula | C8H8N4O4S3 |
| SMILES | O=S(C1=NN=C(S1)NS(=O)(C2=CC=CC=C2)=O)(N)=O |
Summary
Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with K i s of 15 nM, 9 nM, 94 nM and 78 nM for hCA I , hCA II , EcoCAγ and VchCAγ , respectively. Benzolamide also inhibits CAS3 , with a K i of 54 nM. Benzolamide can be used for the research of glaucoma and seizures [1] [2] [3] .
IC50 & Target
In Vitro
Benzolamide inhibits hCA I, hCA II, EcoCAγ and VchCAγ, with K
i
s of 15 nM, 9 nM, 94 nM and 78 nM, respectively
[1]
.
Benzolamide shows selectivity for CAS3 (K
i
=54 nM) over CAS1 (K
i
=2115 nM) and CAS2 (K
i
=410 nM)
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Benzolamide (90 µmol/kg; i.p.) decreases brain pH and suppresses electrographic post-asphyxia seizures in rats
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male and female Wistar Han rats (11-day-old) [3] |
| Dosage: | 90 µmol/kg |
| Administration: | A single i.p. |
| Result: |
Induced a fast brain acidosis of a comparable magnitude.
Suppressed electrographic seizures after asphyxia by slowing down the recovery of brain pH. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04209790 | Geisinger Clinic |
Glioblastoma|Surgery|High Grade Glioma
|
April 1, 2020 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 250 mg/mL ( 780.35 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
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.
Synonyms
