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Darigabat
Catalog No. T16489Cas No. 1614245-70-3
Alias PF-6372865, PF-06372865, CVL-865
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.
Darigabat
Catalog No. T16489Alias PF-6372865, PF-06372865, CVL-865Cas No. 1614245-70-3
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $49 | In Stock |
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Purity:98.89%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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]. |
| Alias | PF-6372865, PF-06372865, CVL-865 |
| Molecular Weight | 440.49 |
| Formula | C22H21FN4O3S |
| Cas No. | 1614245-70-3 |
Storage & Solubility Information
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 30 mg/mL (68.11 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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