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Darigabat

Catalog No. T16489 CAS 1614245-70-3

Synonyms: CVL-865, PF-6372865, PF-06372865

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.

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Darigabat, CAS 1614245-70-3

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2 mg	In stock	$ 68.00

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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.
Targets&IC50	α2 PAM:134 nM(ki), α1 PAM:21 nM(ki), α2:2.9 nM（ki）
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].

Synonyms	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), Sonication is recommended.

References and Literature

1. Owen RM, et al. Design and Identification of a Novel, Functionally Subtype Selective GABAA Positive Allosteric Modulator (PF-06372865). J Med Chem. 2019 Jun 27;62(12):5773-5796.

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Keywords

Darigabat 1614245-70-3 Membrane transporter/Ion channel Neuroscience GABA Receptor CVL-865 PF-6372865 PF 06372865 PF-06372865 PF06372865 inhibitor inhibit

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