DFP00173 is a potent and selective aquaporin-3 (AQP3) inhibitor. DFP00173 is selective for AQP3 over the homologous AQP isoforms AQP7 and AQP9.
DFP00173 inhibits mouse and human AQP3 with an IC50 of ∼0.1-0.4 μM. DFP00173 inhibits the glycerol permeability of human erythrocytes with an IC50 of ~0.2 µM.
| Molecular Weight | 332.16 |
| Formula | C11H7Cl2N3O3S |
| CAS Number | 672286-03-2 |
| Solubility (25°C) | DMSO 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 AQP Products |
|---|
| TC AQP1 1
TC AQP1 1 (m-Phenylenediacrylic acid) is a potent AQP1 inhibitor. TC AQP1 1 inhibits AQP1-mediated water flux in oocytes, with an IC50 of 8 μM. |
| Z433927330
Z433927330 is a potent and selective inhibitor of Aquaporin-7 (AQP7), less potently inhibits AQP3 and AQPs9, with IC50s of ~0.2 µM, ~0.7 µM and ~1.1 µM for mAQP7, mAQP3 and mAQP9, respectively. |
| Bacopaside II
Bacopaside II, an extract from the medicinal herb Bacopa monnieri, blocks the Aquaporin-1 (AQP1) water channel and impairs migration of cells that express AQP1. Bacopaside II induces cell cycle arrest and apoptosis. |
| TGN 020
TGN 020 is a aquaporin 4 (AQP4) channel blocker. |
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