SML0723

ML252

≥98% (HPLC)

• Synonym(e): (S)-2-Phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide
• Empirische Formel (Hill-System): C₂₀H₂₄N₂O
• CAS-Nummer: 1392494-64-2
• Molekulargewicht: 308.42
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: , light to dark purple
• Löslichkeit: DMSO: 25 mg/mL, clear
• Lagertemp.: 2-8°C

Beschreibung

Biochem./physiol. Wirkung

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.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable