ML228 is a potent the HIF pathway activator, with EC50 values of 1.23 and 1.4 μM for HRE gene reporter assay and HIF-1α nuclear translocation assay respectively. ML228 acts via chelation of iron, independently of PHD. ML228 also exhibits > 80% inhibition of the human A3 receptor, dopamine transporter, μ receptor, hERG and 5-HT2B receptor, and rat sodium channel site 2, at a concentration of 10 μM.
| Molecular Weight | 415.49 |
| Formula | C27H21N5 |
| CAS Number | 1357171-62-0 |
| Solubility (25°C) | DMSO ≥ 29 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 HIF Products |
|---|
| 3-Aminobenzoic acid
3-Aminobenzoic acid is a hypoxia-inducible factor-1α (HIF-1α) inhibitor. |
| Steppogenin
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. |
| HIV-IN-7
Axl-IN-16 is a Axl inhibitor. |
| HIF-2α-IN-9
HIF-2α-IN-9 is an inhibitor ofHIF-2α. |
| PHD-IN-2
PHD-IN-2 is a PHD antagonist (IC50: < 5 nM). |
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