ML 252

Product Description

ML 252 is a potent and selective inhibitor of K_V7.2 voltage-gated potassium channels (IC₅₀ = 70 nM), which displays >40-fold selectivity for K_V7.2 over K_V7.1 channels (IC₅₀ = 2.9 μM for K_V7.1). ML 252 is the (S)-enantiomer, and is more potent than the (R)-enantiomer or racemic mixture (IC₅₀ values are 944 and 160 nM, respectively). ML 252 displays selectivity for K_V7.2 over a panel of >68 GPCRs, ion channels and transporters; inhibits melatonin MT₁ receptor 60% at 10 μM. ML 252 is brain penetrant.

Solubility

Preparing Stock Solutions for ML 252

The following data is based on the product molecular weight 308.43

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.24 mL	16.21 mL	32.42 mL
5 mM	0.65 mL	3.24 mL	6.48 mL
10 mM	0.32 mL	1.62 mL	3.24 mL
50 mM	0.06 mL	0.32 mL	0.65 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Cheung Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K_V7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K_V7.2 channel inhibitor. J.Med.Chem. 2012 PMID: 22793372