A2764 dihydrochloride

Name: A2764 dihydrochloride
Brand: MedChemExpress
SKU: HY-135809
Rating: 4.5 (1 reviews)

Cat. No.: HY-135809 Purity: 98.38%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K⁺ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC₅₀=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.

For research use only. We do not sell to patients.

A2764 dihydrochloride Chemical Structure

CAS No. : 861038-72-4

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 82	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 82	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 75	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 6.8 μM (activated mTRESK channel)^[1]

In Vitro

A2764 (100 µM) inhibits the background K⁺ current by 42.8±11.5% when it applies to the oocytes expressing mTRESK^[1].
A2764 (100 µM) shows an improved inhibitory potency for activated channel with an IC₅₀ of activated channel in ionomycin-activated mTRESK current.The subsequent application of A2764 strongly inhibits the current (77.8±3.5%)^[1].
A2764 (100 µM) inhibits the current of TRESK under resting conditions and in the activated state by 42.8±11.5% and 77.8±3.5%, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

351.70

Formula

C₁₅H₂₁Cl₃N₂O

CAS No.

861038-72-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

ClC1=C2C=CC=NC2=C(OCCN(CC)CC)C=C1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : ≥ 100 mg/mL (284.33 mM)

DMSO : 41.67 mg/mL (118.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.8433 mL	14.2167 mL	28.4333 mL
5 mM	0.5687 mL	2.8433 mL	5.6867 mL
10 mM	0.2843 mL	1.4217 mL	2.8433 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.91 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.38%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (249 KB) HNMR (220 KB) LCMS (138 KB)

Handling Instructions (2659 KB)

References

[1]. Lengyel M, et al. Chemically Modified Derivatives of the Activator Compound Cloxyquin Exert Inhibitory Effect on TRESK (K2P18.1) Background Potassium Channel.Mol Pharmacol. 2019 Jun;95(6):652-660. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.8433 mL	14.2167 mL	28.4333 mL	71.0833 mL
	5 mM	0.5687 mL	2.8433 mL	5.6867 mL	14.2167 mL
	10 mM	0.2843 mL	1.4217 mL	2.8433 mL	7.1083 mL
	15 mM	0.1896 mL	0.9478 mL	1.8956 mL	4.7389 mL
	20 mM	0.1422 mL	0.7108 mL	1.4217 mL	3.5542 mL
	25 mM	0.1137 mL	0.5687 mL	1.1373 mL	2.8433 mL
	30 mM	0.0948 mL	0.4739 mL	0.9478 mL	2.3694 mL
	40 mM	0.0711 mL	0.3554 mL	0.7108 mL	1.7771 mL
	50 mM	0.0569 mL	0.2843 mL	0.5687 mL	1.4217 mL
	60 mM	0.0474 mL	0.2369 mL	0.4739 mL	1.1847 mL
	80 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8885 mL
	100 mM	0.0284 mL	0.1422 mL	0.2843 mL	0.7108 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.