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ML133 HCl Potassium Channel inhibitor

Name: ML133 HCl
Brand: Selleck Chemicals
SKU: S2825
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S2825

ML133 HCl is a selective potassium channel inhibitor for K_ir2.1 with IC50 of 1.8 μM (pH 7.4) and 290 nM (pH 8.5), has no effect on K_ir1.1 and weak activity for K_ir4.1 and K_ir7.1.

Chemical Structure

Molecular Weight: 313.82

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.92

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR
Other Potassium Channel Products	Nicorandil TRAM-34 Sophocarpine Hydralazine HCl Gliquidone PAP-1 VU0071063 Apamin A2793 Ajmaline

Solubility

In vitro
Batch:

DMSO : 63 mg/mL (200.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.15mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 63 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.45mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	313.82	Formula	C₁₉H₁₉NO.HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1222781-70-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	COC1=CC=C(C=C1)CNCC2=CC=CC3=CC=CC=C32.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Kir2.1 290 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 K_ir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of K_ir2.1, especially D172 and I176.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21615117/

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