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BL-1249

Name: BL-1249
Brand: TargetMol
SKU: T14666
Price: 48 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14666Cas No. 18200-13-0

BL-1249 is a selective and potent non-steroidal potassium channel activator with anti-inflammatory activity that activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2).

BL-1249

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Purity: 98.25%

Catalog No. T14666Cas No. 18200-13-0

BL-1249 is a selective and potent non-steroidal potassium channel activator with anti-inflammatory activity that activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$48	In Stock	In Stock
5 mg	$113	In Stock	In Stock
10 mg	$179	In Stock	In Stock
25 mg	$272	In Stock	In Stock
50 mg	$372	In Stock	In Stock
100 mg	$653	-	In Stock
500 mg	$1,350	-	In Stock
1 mL x 10 mM (in DMSO)	$157	In Stock	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.25%

Appearance:Solid

Color:Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	BL-1249 is a selective and potent non-steroidal potassium channel activator with anti-inflammatory activity that activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2).
Targets&IC50	TREK2:8.0 μM (EC50), TREK1:5.5 μM (EC50), Smooth muscle cells (SMCs):21.0 μM (Human, EC50)
In vitro	Evaluated by a decrease in fluorescence of the voltage-sensitive dye bis(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 = 1.26 +/- 0.6 μM) or direct electrophysiological measurements (EC50 = 1.49 +/- 0.08 μM), BL-1249 demonstrates concentration-dependent membrane depolarization in cultured human bladder smooth muscle cells[2]. Patch clamp experiments indicate that, akin to a diverse range of other TREK subfamily gating signals, BL-1249 stimulates a selective screening 'C-type' gate that controls K2P functionality. BL-1249 exhibits selectivity within the TREK subfamily, activating K2P2.1 (TREK-1) and K2P10.1 (TREK-2) approximately 10 times more actively than K2P4.1 (TRAAK). Studies on mutants and K2P2.1 (TREK-1)/K2P4.1 (TRAAK) chimeras highlight the critical role of the C-terminal tail in the action of BL-1249, and identify the M2/M3 transmembrane helix interface as a key site of BL-1249 selectivity[1].
In vivo	In an anesthetized rat model, BL-1249 (1 mg/kg i.v.) decreased the number of isovolumic contractions, without significantly affecting blood pressure. Thus, BL-1249 behaves as a potassium channel activator that exhibits bladder versus vascular selectivity both in vitro and in vivo[2].

Chemical Properties

Molecular Weight	291.35
Formula	C₁₇H₁₇N₅
Cas No.	18200-13-0
Smiles	C1CCc2c(C1)cccc2Nc1ccccc1-c1nnn[nH]1
Relative Density.	1.291g/cm3

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: 30 mg/mL (102.97 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.86 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	3.4323 mL	17.1615 mL	34.3230 mL	171.6149 mL
5 mM	0.6865 mL	3.4323 mL	6.8646 mL	34.3230 mL
10 mM	0.3432 mL	1.7161 mL	3.4323 mL	17.1615 mL
20 mM	0.1716 mL	0.8581 mL	1.7161 mL	8.5807 mL
50 mM	0.0686 mL	0.3432 mL	0.6865 mL	3.4323 mL
100 mM	0.0343 mL	0.1716 mL	0.3432 mL	1.7161 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