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RL648_81

Name: RL648_81
Brand: TargetMol
SKU: T28544
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T28544Cas No. 1919050-87-5

RL648_81 is a selective activator of KCNQ2/3 channels (EC50 = 190 nM). RL648_81 can be used in studies about neuronal hyperexcitability neurologic disorders.

RL648_81

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Purity: 99.82%

Catalog No. T28544Cas No. 1919050-87-5

RL648_81 is a selective activator of KCNQ2/3 channels (EC50 = 190 nM). RL648_81 can be used in studies about neuronal hyperexcitability neurologic disorders.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$35	In Stock	In Stock
10 mg	$64	In Stock	In Stock
25 mg	$143	In Stock	In Stock
50 mg	$212	In Stock	In Stock
100 mg	$298	-	In Stock
1 mL x 10 mM (in DMSO)	$42	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.82%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

RL648_81 AI Summary

RL648_81 exhibits agonist activity on various Kv7 channels expressed in different cell lines, as demonstrated by whole-cell patch clamp electrophysiology assays. Specifically, it has an EC50 of 190.0 nM for human Kv7.2/7.3 channels in CHO cells and an EC2 ranging from 0.09 µM to 0.29 µM for different Kv7 channels in HEK293 cells. In particular, the compound has an EC2 of 0.1 µM for human Kv7.4 and an EC2 of 0.09 µM for human Kv7.4/7.5. Additionally, it exhibits selectivity with a selectivity index of 0.3 between Kv7.2/7.3 and Kv7.4/7.5 channels and a half-life of 5.733 hours in human liver microsomes. Moreover, in the SyncroPatch assay, at a 5 µM concentration, RL648_81 shifts the voltage-dependent activation of the Kv7.2 channel to more negative potentials, with a V1/2 value of -48.1 mV for Kv7.2 and 1.9 mV for the Kv7.2 W236L mutant. The compound demonstrates a dose-dependent response, increasing maximum current density and showing EC50 values ranging from 240.0 nM to 4000.0 nM, indicating a stimulatory effect on Kv7.2/7.3 channel activity..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

RL648_81 is a selective activator of KCNQ2/3 channels (EC50 = 190 nM). RL648_81 can be used in studies about neuronal hyperexcitability neurologic disorders.

Chemical Properties

Molecular Weight	371.33
Formula	C₁₇H₁₇F₄N₃O₂
Cas No.	1919050-87-5
Smiles	CCOC(=O)Nc1ccc(NCc2ccc(cc2)C(F)(F)F)c(F)c1N
Relative Density.	1.398 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 27.5 mg/mL (74.06 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+90% Corn Oil: 2 mg/mL (5.39 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6930 mL	13.4651 mL	26.9302 mL	134.6511 mL
5 mM	0.5386 mL	2.6930 mL	5.3860 mL	26.9302 mL
10 mM	0.2693 mL	1.3465 mL	2.6930 mL	13.4651 mL
20 mM	0.1347 mL	0.6733 mL	1.3465 mL	6.7326 mL
50 mM	0.0539 mL	0.2693 mL	0.5386 mL	2.6930 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc