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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $57 | In Stock | |
10 mg | $96 | In Stock | |
25 mg | $210 | In Stock | |
50 mg | $347 | In Stock | |
100 mg | $513 | In Stock | |
500 mg | $1,080 | In Stock | |
1 mL x 10 mM (in DMSO) | $57 | In Stock |
Description | ML335 is a selective activator of TREK-1 and TREK-2. |
In vitro | Xenopus oocyte two-electrode voltage-clamp measurements indicate that ML335 and ML402 activate K2P2.1 and K2P10.1, but not K2P4.1 (14.3±2.7 μM for K2P2.1-ML335; 13.7±7.0 μM for K2P2.1-ML402; 5.2±0.5 μM for K2P10.1-ML335; and 5.9±1.6 μM for K2P10.1-ML402). Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a reversed phenotype for ML335 and ML402 activation. ML335 and ML402 also activate K2P2.1 in HEK293 cells in a manner similar to their effects in Xenopus oocytes (5.2±0.8 μM and 5.9±1.6 μM for ML335 and ML402, respectively [n≥3]). |
Cell Research | Mouse K2P2.1, human K2P4.1, and mutants are expressed from a previously described pIRES2-EGFP vector in HEK293T cells (ATTC). 70% confluent cells are transfected (in 35-mm diameter wells) with LipofectAMINE 2000 for 6?h, and plated onto coverslips coated with Matrigel. Effects of ML335, ML402 and arachidonic acid on K2P2.1 current at 0?mV are measured by whole-cell patch-clamp experiments 24?h after transfection. Acquisition and analysis are performed using pCLAMP9 and an Axopatch 200B amplifier. Pipette resistance ranges from 1 to 1.5?MΩ. Pipette solution contains the following: 145?mM KCl, 3?mM MgCl2, 5?mM EGTA and 20?mM HEPES (pH 7.2 with KOH). Bath solution contains the following: 145?mM NaCl, 5?mM KCl, 1?mM CaCl2, 3?mM MgCl2 and 20?mM HEPES (pH 7.4 with NaOH). K2P2.1 currents are elicited by a 1?s ramp from -100 to +50?mV from a -80?mV holding potential. After stabilization of the basal current, ML335 and ML402 are perfused at 200?mL per hour until potentiation is stably reached[1]. |
Molecular Weight | 373.25 |
Formula | C15H14Cl2N2O3S |
Cas No. | 825658-06-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (120.56 mM) ![]() | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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