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Darigabat

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

🥰Excellent

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

🥰Excellent

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. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.29%

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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	α2:2.9 nM（ki）, α2 PAM:134 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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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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