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Description: Potent and selective KV7.2 inhibitor; brain penetrant
Chemical Name: (S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide
Purity: ≥98% (HPLC)
Biological Activity for ML 252
ML 252 is a potent and selective inhibitor of KV7.2 voltage-gated potassium channels (IC50 = 70 nM), which displays >40-fold selectivity for KV7.2 over KV7.1 channels (IC50 = 2.9 μM for KV7.1). 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 KV7.2 over a panel of >68 GPCRs, ion channels and transporters; inhibits melatonin MT1 receptor 60% at 10 μM. ML 252 is brain penetrant.
Compound Libraries for ML 252
ML 252 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for ML 252
| M. Wt | 308.43 |
| Formula | C20H24N2O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1392494-64-2 |
| PubChem ID | 26873419 |
| InChI Key | FROGGFONBYACJB-UHFFFAOYSA-N |
| Smiles | O=C([C@@H](CC)C1=CC=CC=C1)NC2=C(N3CCCC3)C=CC=C2 |
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.
Solubility Data for ML 252
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 30.84 | 100 | |
| ethanol | 30.84 | 100 |
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 will affect the solvent volumes required to prepare stock solutions.
| 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 |
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Product Datasheets for ML 252
References for ML 252
References are publications that support the biological activity of the product.
Cheung et al (2012) Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of KV7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phe J.Med.Chem. 55 6975 PMID: 22793372
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Citations for ML 252
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