ML252

ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant [1][2].

Product Specifications

CAS Number

[1392494-64-2]

UNSPSC

12352005

Target

Cytochrome P450; Potassium Channel

Type

Reference compound

Related Pathways

Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/ml252.html

Purity

99.9

Solubility

DMSO : 100 mg/mL (ultrasonic; warming)

Smiles

O=C(NC1=CC=CC=C1N2CCCC2)[C@H](C3=CC=CC=C3)CC

Molecular Formula

C20H24N2O

Molecular Weight

308.42

References & Citations

[1]Yu H, et al. Identification of a novel, small molecule inhibitor of KCNQ2 channels. 2011 Oct 28 [updated 2013 Feb 25]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD) : National Center for Biotechnology Information (US) ; 2010–. |[2]Cheung YY, et al. Discovery of a series of 2-phenyl-N- (2- (pyrrolidin-1-yl) phenyl) acetamides as novel molecular switches that modulate modes of K (v) 7.2 (KCNQ2) channel pharmacology: identification of (S) -2-phenyl-N- (2- (pyrrolidin-1-yl) phenyl) butanamide (ML252) as a potent, brain penetrant K (v) 7.2 channel inhibitor. J Med Chem. 2012 Aug 9;55 (15) :6975-9.