Darigabat (Synonyms: PF-06372865; CVL-865)

Name: Darigabat
Brand: MedChemExpress
SKU: HY-120874
Rating: 4.5 (0 reviews)

Cat. No.: HY-120874 Pureza: 99.29%: Ficha de datos
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Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABA_A positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABA_A receptors containing α1/α2/α3/α5 subunits (K_is of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy.

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Darigabat Estructura química

No. CAS : 1614245-70-3

Tamaño	Stock	Cantidad

Muestra gratis (0.1 - 0.2 mg)	Solicite ahora
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
200 mg	Obtener un presupuesto
500 mg	Obtener un presupuesto

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Descripciòn

IC₅₀ & Target

Ki: 2.9 nM (α2), 21 nM (α1 PAM) and 134 nM (α2 PAM)^[1]

In Vitro

Darigabat (compound 34) has K_i values of 0.18 nM, 2.9 nM, 1.1 nM, 18 nM for human GABA_A α1β3γ2, α2β2γ2, α3β3γ2, α5β2γ2 and 0.34 nM, 4.58 nM for rat GABA_A α1β3γ2, α2β2γ2^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Darigabat (compound 34; 3, 10 mg/kg; orally; single dose) significantly increases the paw withdrawal threshold (PWT) in chronic constriction injury (CCI) animals^[1].
Darigabat (0.3, 3, 10 mg/kg for mouse and 1, 3, 10 mg/kg for rat; orally) exhibits efficacy in two models of epilepsy, PTZ induced seizures (mouse), and amygdala kindling (rat)^[1].
Darigabat (0.1, 0.32, 1, 3.2 and 10 mg/kg; orally) has anxiolytic activity at 3.2 and 10 mg/kg in elevated plus maze (male C57Bl/6 mice)^[1].
Darigabat has a T_1/2 of 1.1 hours, a Cl_p of 22 mL/min/kg, and a V_ss of 2.1 L/kg for rats^[1].
Darigabat has a T_1/2 of 0.9 hours, a Cl_p of 29 mL/min/kg, and a V_ss of 3.4 L/kg for dogs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Chronic constriction injury (CCI) model (male Wistar rats)^[1]
Dosage:	3, 10 mg/kg
Administration:	Orally
Result:	Significantly increased paw withdrawal latency.

Ensayo clínico

Peso molecular

440.49

Fòrmula

C₂₂H₂₁FN₄O₃S

No. CAS

1614245-70-3

Appearance

Solid

Color

Off-white to yellow

SMILES

CCN1C2=NN=CC(C(C=C3)=CC(C(C=CC([S](CC)(=O)=O)=C4)=C4OC)=C3F)=C2N=C1

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (113.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2702 mL	11.3510 mL	22.7020 mL
5 mM	0.4540 mL	2.2702 mL	4.5404 mL
10 mM	0.2270 mL	1.1351 mL	2.2702 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.29%

Select Batch:

Ficha de datos (277 KB) SDS (252 KB)

COA (252 KB) LCMS (95 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2702 mL	11.3510 mL	22.7020 mL	56.7550 mL
	5 mM	0.4540 mL	2.2702 mL	4.5404 mL	11.3510 mL
	10 mM	0.2270 mL	1.1351 mL	2.2702 mL	5.6755 mL
	15 mM	0.1513 mL	0.7567 mL	1.5135 mL	3.7837 mL
	20 mM	0.1135 mL	0.5675 mL	1.1351 mL	2.8377 mL
	25 mM	0.0908 mL	0.4540 mL	0.9081 mL	2.2702 mL
	30 mM	0.0757 mL	0.3784 mL	0.7567 mL	1.8918 mL
	40 mM	0.0568 mL	0.2838 mL	0.5675 mL	1.4189 mL
	50 mM	0.0454 mL	0.2270 mL	0.4540 mL	1.1351 mL
	60 mM	0.0378 mL	0.1892 mL	0.3784 mL	0.9459 mL
	80 mM	0.0284 mL	0.1419 mL	0.2838 mL	0.7094 mL
	100 mM	0.0227 mL	0.1135 mL	0.2270 mL	0.5675 mL

Darigabat Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Darigabat (Synonyms: PF-06372865; CVL-865)

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Darigabat Related Antibodies

Recomendaciones destacadas

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Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Darigabat Related Classifications

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