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Selective K2P2.1 (TREK-1; KCNK2) and K2P10.1 (TREK-2; KCNK10) activator (EC50 values of 14.3 μM and 5.2 μM, respectively); directly stimulates the C-type gate via the K2P modulator pocket. Does not activate K2P4.1 (TRAAK).
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 373.25. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.68 mL||13.4 mL||26.79 mL|
|5 mM||0.54 mL||2.68 mL||5.36 mL|
|10 mM||0.27 mL||1.34 mL||2.68 mL|
|50 mM||0.05 mL||0.27 mL||0.54 mL|
References are publications that support the biological activity of the product.
Pope et al (2018) Protein and chemical determinants of BL-1249 action and selectivity for K2P channels. ACS Chem.Neurosci. 9 3153 PMID: 30089357
Gada et al (2019) Two-pore domain potassium channels: emerging targets for novel analgesic drugs: IUPHAR Review 26. Br.J.Pharmacol. 176 256 PMID: 30325008
Lolicato et al (2017) K2P2.1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site. Nature 547 364 PMID: 28693035
Schewe et al (2019) A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels. Science 363 875 PMID: 30792303
If you know of a relevant reference for ML 335, please let us know.
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Literature in this Area
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.