Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM. Acetazolamide also inhibits hCA II with an IC50 of 130 nM. In vivo, Acetazolamide (40 mg/kg) significantly potentiates the inhibitory effect of MS-275 on tumorigenesis in neuroblastoma (NB) SH-SY5Y xenografts.
| Cell Experiment | |
|---|---|
| Cell lines | renal carcinoma cell lines(Caki-1, Caki-2, ACHN, and A-498) |
| Preparation method | The invasion assay is performed in a Biocoat Matrigel invasion chamber. Cells (n = 1.8 × 105) are added to the chamber and cultured for 48 h in the presence or absence of acetazolamide, which was administered twice during the 48-h period: the first dose at the beginning of the assay and the second after 24 h. After growing for 48 h, noninvasive cells are removed from the upper surface of the membrane with a cotton swab. The invasive cells on the lower surface of the membrane are fixed with 4% (vol/vol) neutral-buffered formaldehyde, stained with toluidine blue, and counted in 20 separate areas with a Leitz Diaplan microscope. |
| Concentrations | 10 μM |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague-Dawley rats |
| Formulation | - |
| Dosages | 10, 100, 200 mg/kg |
| Administration | i.p. |
| Molecular Weight | 222.25 |
| Formula | C4H6N4O3S2 |
| CAS Number | 59-66-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 25 mg/mL |
| Storage | 2-8°C, dry, protect from light, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Carbonic Anhydrase Products |
|---|
| Acetazolamide sodium
Acetazolamide sodium is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM for hCA IX.Acetazolamide reduces the production of intraocular aqueous humor and may be used in glaucoma-related studies. |
| WES-1
WES-1 is an inhibitor of carbonic anhydrase IX (Ki: 55.9 μM). |
| CA inhibitor 2
CA inhibitor 2 is a carbonic anhydrase inhibitor (IC50: 0.033 μM). |
| hCA XII-IN-6
hCA XII-IN-6 is a potent hCA XII inhibitor with a Ki value of 84.2 nM. |
| Carbonic anhydrase inhibitor 15
Carbonic anhydrase inhibitor 15 is a carbonic anhydrase inhibitor (Ki: 8.5 nM for hCA II). |
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