ML252

CAT: 0804-HY-18063-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-18063-01Size:5 mg
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Description
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].
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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, protect from light, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CYP1; CYP2; CYP3; Voltage-gated potassium channel

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