ML402 MedChemExpress (MCE)

Product Name	ML402
Synonyms	ML402;ML 402;ML-402 ;298684-44-3;2-Thiophenecarboxamide, N-[2-(4-chloro-2-methylphenoxy)ethyl]-
CAS	298684-44-3
EINECS
Chemical Formula	C14H14ClNO2S
Molecular Weight	295.78
inchi
Package	10 mM * 1 mL;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	ML402 ML402 MedChemExpress (MCE) HY-104027 298684-44-3 99.86% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions ML402 ML402 MedChemExpress (MCE) HY-104027 298684-44-3 99.86% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. ML402, a thiophene-carboxamide, is a selective K2P2.1(TREK-1) and K2P10.1(TREK-2) activator. ML402 is inactive against K2P4.1(TRAAK). Xenopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1 and K2P10.1 but not K2P4.1(14.3±2.7 μM, K2P2.1-ML335 13.7±7.0 μM, K2P2.1-ML402 5.2±0.5 μM, K2P10.1-ML335 and 5.9±1.6 μM, K2P10.1-ML402). The K2P modulator pocket has a single difference among TREK subfamily members at the cation-π interaction position, K2P2.1 Lys271, which is also a lysine in K2P10.1 but a glutamine in K2P4.1. Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K271Q) is insensitive to ML335 and ML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50 to K2P2.1 (14.3±2.7 μM, K2P2.1-ML335 16.2±3.0 μM, K2P4.1(Q258K)-ML335 13.7±7.0 μM, K2P2.1-ML402 13.6±1.5 μM, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1[1]. K2P2.1cryst ML335 and ML402 complex crystals grow in the same conditions as K2P2.1cryst, but the protein is incubated for at least 1 h with 2.5 mM of activator (including ML 402) before setting the crystal plates. ML335 and ML402 are insoluble in aqueous solutions, so they are dissolved in 100% DMSO at a concentration of 500 mM. Then each compound is diluted 1:100 in SEC buffer to 5 mM concentration, giving a milky solution. This solution is mixed 1:1 to K2P2.1cryst previously concentrating to 12 mg/mL. The K2P2.1cryst ML402 mixture results in a clear solution, while the mixture with ML335 is slightly milky. The samples are briefly centrifuged in a table-top centrifuge (10,000×g) to remove any insoluble material before setting the crystal plates. Dose-response experiments are carried by first preparing a DMSO stock solution of each activator (including ML402) at a concentration of 100 mM. Owing to the low solubility of the compounds the highest test concentrations in recording solution are 100 μM and 80 μM for ML335 and ML402, respectively. Other concentrations are prepared by serial dilutions of the 100 μM solution in recording buffer supplementing with 0.1% DMSO[1]. TREK-1/2[1] In Vitro Xenopus oocyte two-electrode voltage-clamp measurements show that ML335 and ML402 activate K2P2.1 and K2P10.1 but not K2P4.1(14.3±2.7 μM, K2P2.1-ML335 13.7±7.0 μM, K2P2.1-ML402 5.2±0.5 μM, K2P10.1-ML335 and 5.9±1.6 μM, K2P10.1-ML402). The K2P modulator pocket has a single difference among TREK subfamily members at the cation-π interaction position, K2P2.1 Lys271, which is also a lysine in K2P10.1 but a glutamine in K2P4.1. Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. K2P2.1 (K271Q) is insensitive to ML335 and ML402, whereas K2P4.1 (Q258K) responds to both with a similar EC50 to K2P2.1 (14.3±2.7 μM, K2P2.1-ML335 16.2±3.0 μM, K2P4.1(Q258K)-ML335 13.7±7.0 μM, K2P2.1-ML402 13.6±1.5 μM, K2P4.1 (Q258K)-ML402) but with a lower magnitude response than K2P2.1[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ML402 Related Antibodies \| \| \| \| \| \| \| \| \| \| [1]. Lolicato M, et al. K2P2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature. 2017 Jul 20 547(7663):364-368. [Content Brief]
Supplier Website	https://www.medchemexpress.com/ML402.html
Last Update	2025-05-21 16:50:25

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