Home Transmembrane Transporters Potassium Channel inhibitor ML133 HCl For research use only.

ML133 HCl

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

ML133 HCl Chemical Structure

CAS: 1222781-70-5

Selleck's ML133 HCl has been cited by 4 publications

Purity & Quality Control

Batch: S282501 DMSO] 63 mg/mL] false] Ethanol] 6 mg/mL] false] Water] Insoluble] false Purity: 99.92%
99.92

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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
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]

Chemical Information & Solubility

Molecular Weight 313.82 Formula

C19H19NO.HCl
CAS No. 1222781-70-5 SDF Download ML133 HCl SDF
Smiles COC1=CC=C(C=C1)CNCC2=CC=CC3=CC=CC=C32.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 63 mg/mL ( (200.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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