| Bioactivity | ML335 is a selective activator of both TREK-1 and TREK-2. | ||||||||||||||||||||||||||||||
| Target | TREK-1, TREK-2| Invitro |
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). Swapping the Lys271 equivalent between K2P2.1 and K2P4.1 results in a clear phenotype reversal for ML335 and M402 activation. ML335 and ML402 activate K2P2.1 in HEK293 cells 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))[1]. |
Name |
ML335 |
CAS |
825658-06-8 |
Formula |
C15H14Cl2N2O3S |
Molar Mass |
373.25 |
Appearance |
Solid |
Transport |
Room temperature in continental US; may vary elsewhere. |
Storage |
Reference |
[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. |
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