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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $53 | In Stock | |
1 mL x 10 mM (in DMSO) | $95 | In Stock |
Description | Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy. |
In vitro | PF-06372865 (Compound 34) co-applied with equimolar concentrations of GABA showed Ki values of 0.18 nM, 2.9 nM, 1.1 nM, and 18 nM for human GABAA α1β3γ2, α2β2γ2, α3β3γ2, and α5β2γ2, respectively[1]. |
In vivo | In the maximal electroshock seizure (MES) model in rats, PF-06372865 at both doses of 3 and 10 mg/kg significantly increased the hindlimb withdrawal latency. In the pentylenetetrazole (PTZ) seizure model in mice, PF-06372865 at all doses of 0.3, 3, and 10 mg/kg significantly increased the seizure onset latency[1]. |
Alias | CVL-865, PF-6372865, PF-06372865 |
Molecular Weight | 440.49 |
Formula | C22H21FN4O3S |
Cas No. | 1614245-70-3 |
Storage | keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (68.11 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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