2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. A2764 dihydrochloride

A2764 dihydrochloride 

Cat. No.: HY-135809 Purity: 98.38%
COA Handling Instructions

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

A2764 dihydrochloride Chemical Structure

CAS No. : 861038-72-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 132 In-stock
Solid
10 mg USD 120 In-stock
50 mg USD 350 In-stock
100 mg USD 550 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

351.70

Appearance

Solid

Formula

C15H21Cl3N2O
CAS No.
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)

*"≥" 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

A2764861038-72-4A 2764A-2764Potassium ChannelKcsATRESKcurrentK+ migrainenociceptionInhibitorinhibitorinhibit

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A2764 dihydrochloride
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