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PF-06372865 

Cat. No. M28688

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PF-06372865  Structure
Synonym:

Darigabat

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
References

[1] Rok Cerne, et al. Pharmacol Ther. GABAkines - Advances in the discovery, development, and commercialization of positive allosteric modulators of GABAA receptors

[2] Rachel Gurrell, et al. Clin Pharmacol Drug Dev. Safety, Tolerability, and Pharmacokinetics of Multiple Repeated Oral Doses of the α2/3/5-Subtype Selective GABAA -Positive Allosteric Modulator PF-06372865 in Healthy Volunteers

[3] Guido van Amerongen, et al. Br J Anaesth. Analgesic potential of PF-06372865, an α2/α3/α5 subtype-selective GABAA partial agonist, in humans

[4] Rachel Gurrell, et al. Neurology. Photosensitive epilepsy: Robust clinical efficacy of a selective GABA potentiator

[5] Venceslas Duveau, et al. CNS Neurosci Ther. Pronounced antiepileptic activity of the subtype-selective GABAA -positive allosteric modulator PF-06372865 in the GAERS absence epilepsy model

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06372865 , Darigabat supplier, GABA Receptor, inhibitors, activators

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