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Darigabat

Name: Darigabat
Brand: TargetMol
SKU: T16489
Price: 49 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.29%

Catalog No. T16489Alias PF-6372865, PF-06372865, CVL-865Cas No. 1614245-70-3

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
1 mg	$49	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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.

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Batch Information

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Purity:99.29%

Appearance:Solid

Color:White to Yellow

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COA

Product Introduction

Bioactivity

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), α2:2.9 nM（ki）, α1 PAM:21 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	PF-6372865, PF-06372865, CVL-865

Chemical Properties

Molecular Weight	440.49
Formula	C₂₂H₂₁FN₄O₃S
Cas No.	1614245-70-3
Smiles	CCn1cnc2c(cnnc12)-c1ccc(F)c(c1)-c1ccc(cc1OC)S(=O)(=O)CC
Relative Density.	1.35 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 30 mg/mL (68.11 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.54 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2702 mL	11.3510 mL	22.7020 mL	113.5100 mL
5 mM	0.4540 mL	2.2702 mL	4.5404 mL	22.7020 mL
10 mM	0.2270 mL	1.1351 mL	2.2702 mL	11.3510 mL
20 mM	0.1135 mL	0.5675 mL	1.1351 mL	5.6755 mL
50 mM	0.0454 mL	0.2270 mL	0.4540 mL	2.2702 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc