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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
|Source||Front Cell Neurosci (2015). Figure 3.ML133|
|Method||CyQUANT proliferation assay|
|Cell Lines||Microglial cells|
|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|
Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133.
Wang HR, et al. ACS Chem Biol. 2011 Aug 19;6(8):845-56. PMID: 21615117.
A potent and selective small molecule Kir2.1 inhibitor.
Wu M, et al. Probe Reports from the NIH Molecular Libraries Program [Internet]. 2010 Feb 26. PMID: 21433384.
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