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PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
| Molecular Weight | 440.49 |
| Formula | C22H21FN4O3S |
| CAS Number | 1614245-70-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic) |
| Storage | 4°C, protect from light |
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