Darigabat
Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM) . Darigabat 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. Darigabat can across the blood-brain barrier (BBB) . Darigabat has anxiolytic activity and has the potential for epilepsy[1].
Product Specifications
CAS Number
[1614245-70-3]
Product Name Alternative
PF-06372865; CVL-865
UNSPSC
12352005
Target
GABA Receptor
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/pf-06372865.html
Purity
99.29
Solubility
DMSO : 50 mg/mL (ultrasonic)
Smiles
CCN1C2=NN=CC(C(C=C3)=CC(C(C=CC([S](CC)(=O)=O)=C4)=C4OC)=C3F)=C2N=C1
Molecular Formula
C22H21FN4O3S
Molecular Weight
440.49
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Available Sizes
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