ML133 HCl

Catalog No.S2825

For research use only.

ML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.

ML133 HCl Chemical Structure

CAS No. 1222781-70-5

Selleck's ML133 HCl has been cited by 2 Publications

Purity & Quality Control

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Biological Activity

Description ML133 HCl is a selective potassium channel inhibitor for Kir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on Kir1.1 and weak activity for Kir4.1 and Kir7.1.
Targets
Kir2.1 [1]
290 nM
In vitro

The ratio of total concentration of extracellular ML133 versus intracellular ML133 is 1:0.13 at pH 6.5, 1:9.09 at pH 8.5. ML133 is clean against 3A4 and 2C9 (IC50 >30 μM), displays moderate inhibition of 1A2 (IC50 = 3.3 μM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 μM) in CYP450 assay. ML133 is highly protein bound (>99%) in both human and rat and also displays high intrinsic clearance in both species. ML133 (10 μM) is not displaced by K+ influx from the wild-type Kir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of Kir2.1, especially D172 and I176. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 313.82
Formula

C19H19NO.HCl

CAS No. 1222781-70-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=CC=C(C=C1)CNCC2=CC=CC3=CC=CC=C32.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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