ML133 hydrochloride is a potent K(ir)2.1 inhibitor, which inhibits K(ir)2.1 with an IC50 of 1.8 μM at pH 7.4 and 290 nM at pH 8.5 but exhibits little selectivity against other members of Kir2.x family channels. ML133 hydrochloride has no effect on K(ir)1.1 (IC50 > 300 μM) and displays weak activity for K(ir)4.1 (76 μM) and K(ir)7.1 (33 μM). ML133 HCl also displays modest selectivity versus hERG and possesses fair ancillary pharmacology against a larger panel of GPCRs, ion channels and transporters.
Hua Xi Kou Qiang Yi Xue Za Zhi. 2022 Apr;40(2): 139–147.
Effect of inward rectifier potassium 2.1 channel on the osteogenic differentiation of human dental follicle cells and its mechanism
ML133 hydrochloride purchased from AbMole
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Source | Front Cell Neurosci (2015). Figure 3.ML133 |
| Method | CyQUANT proliferation assay | |
| Cell Lines | Microglial cells | |
| Concentrations | 20 μM | |
| Incubation Time | 24 h | |
| Results | Because both Kir2.1 blockers (Ba2+, ML133) greatly reduced migration, we asked whether their morphology changed to that of LPS-stimulated cells. It did not; and blocking Kir2.1 did not obviously affect their unipolar morphology under any of the activation states examined |
| Molecular Weight | 313.82 |
| Formula | C19H19NO.HCl |
| CAS Number | 1222781-70-5 |
| Solubility (25°C) | DMSO 48 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.
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