ML252
SIGMA/SML0723 - ≥98% (HPLC)
Synonym: (S)
CAS Number: 1392494-64-2
Empirical Formula (Hill Notation): C20H24N2O
Molecular Weight: 308.42
Linear Formula: C20H24N2O
Product Type: Chemical
assay | ≥98% (HPLC) |
color | , light to dark purple |
form | powder |
Quality Level | 100 |
solubility | DMSO: 25 mg/mL, clear |
storage temp. | 2-8°C |
Biochem/physiol Actions: | ML252 is a potent, brain penetrant potassium channel Kv7.2 (KCNQ2) inhibitor with an IC50 of 69 nM. ML252 is only slightly selective over KCNQ3 and KCNQ4 but is over 40-fold selective for KCNQ2 vs KCNQ1, unlike other KCNQ inbhibitors currently used. ML252 was also selective vs. >68 tested GPCRs, ion channels, and transporters. Potassium channel Kv7.2 has become a new target for Alzheimer′s Disease drug research because inhibiting it enhances acetylcholine release. SAR studies showed a small structural change from ethyl group to hydrogen resulted in a functional shift from antagonist to agonist activity (37, EC50 of 170 nM), suggesting an interaction at a critical site for controlling KCNQ2 channel gating. |
Packaging: | 5, 25 mg in glass bottle |
RIDADR | NONH for all modes of transport |
WGK Germany | WGK 3 |
Flash Point(F) | Not applicable |
Flash Point(C) | Not applicable |
Purity | ≥98% (HPLC) |
Storage Temp. | 2-8°C |
UNSPSC | 12352200 |