2. GPCR/G Protein Neuronal Signaling
  3. Dopamine Receptor
  4. GSK598809

GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.

Para uso exclusivo en investigación. No vendemos a pacientes.

GSK598809

GSK598809 Estructura química

No. CAS : 863680-45-9

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

* Seleccione Cantidad antes de agregar artículos.

This product is a controlled substance and not for sale in your territory.

Revisión del cliente

Based on 1 publication(s) in Google Scholar

Other Forms of GSK598809:

GSK598809 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE GSK598809

Ver todos los productos específicos de isoformas Dopamine Receptor:

Ver todas las isoformas
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

  • Actividad biológica

  • Protocolo

  • Pureza y Documentación

  • Referencias

  • Revisión del cliente

Descripciòn

GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.

IC50 & Target

D3 Receptor

 

In Vivo

Cocaine and GSK598809 each increases peak mean arterial blood pressure. Least square mean differences are significant for both doses of cocaine compared with its vehicle. Likewise, least square mean differences are significant for both doses of GSK598809 as compared with its vehicle. The experimental question of interest, that is, whether GSK598809 significantly increases cocaine effects on peak mean arterial blood pressure, is probed by a prior it tests on the means of the fitted regression model. The dose of 3 mg/kg GSK598809 significantly increases the pressor effects of 5.6 mg/kg cocaine and of 1.7 mg/kg cocaine[1].

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

481.51

Fòrmula

C22H23F4N5OS
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

CC1=C(C2=NN=C(SCCCN3CC4(C5=CC=C(C(F)(F)F)C=C5F)CC4C3)N2C)OC=N1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 83.33 mg/mL (173.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

1M HCl : 28.57 mg/mL (59.33 mM; ultrasonic and adjust pH to 2 with HCl)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0768 mL 10.3840 mL 20.7680 mL
5 mM 0.4154 mL 2.0768 mL 4.1536 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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).
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
Referencias
Administraciòn de animales
[1]

Dogs[1]
Male beagle dogs are used throughout the study. The experiment is conducted in phases. In the first (hemodynamics) phase, the dogs are dosed at weekly intervals over a period of 9 weeks with combinations of either GSK598809 or vehicle, followed by either cocaine or vehicle. After the baseline measurements are recorded, technical staff briefly returns to the animal room to administer GSK598809 (or vehicle) to all the dogs via oral gavage and activate the timers on the preloaded and preprogrammed infusion pumps[1].

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
1M HCl / DMSO 1 mM 2.0768 mL 10.3840 mL 20.7680 mL 51.9200 mL
5 mM 0.4154 mL 2.0768 mL 4.1536 mL 10.3840 mL
10 mM 0.2077 mL 1.0384 mL 2.0768 mL 5.1920 mL
15 mM 0.1385 mL 0.6923 mL 1.3845 mL 3.4613 mL
20 mM 0.1038 mL 0.5192 mL 1.0384 mL 2.5960 mL
25 mM 0.0831 mL 0.4154 mL 0.8307 mL 2.0768 mL
30 mM 0.0692 mL 0.3461 mL 0.6923 mL 1.7307 mL
40 mM 0.0519 mL 0.2596 mL 0.5192 mL 1.2980 mL
50 mM 0.0415 mL 0.2077 mL 0.4154 mL 1.0384 mL
DMSO 60 mM 0.0346 mL 0.1731 mL 0.3461 mL 0.8653 mL
80 mM 0.0260 mL 0.1298 mL 0.2596 mL 0.6490 mL
100 mM 0.0208 mL 0.1038 mL 0.2077 mL 0.5192 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

GSK598809 Related Classifications

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.

Keywords:

GSK598809863680-45-9GSK 598809GSK-598809Dopamine ReceptorInhibitorinhibitorinhibit

Productos vistos recientemente:

Consulta en línea

Your information is safe with us. * Required Fields.

Nombre del producto

  

Requested Quantity *

Nombre del solicitante *

 

Saludo

Direcciòn del E-mail *

 

Número de teléfono *

Department

 

Nombre de la Organizaciòn *

City

Provincia

Country or Region *

      

Observaciones

Consulta para venta a granel

Inquiry Information

Nombre del producto:
GSK598809
Cat. No.:
HY-19654
Cantidad:
MCE Japan Authorized Agent:

Revisión del cliente

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Nombre del producto

  

Lot #

Nombre del solicitante *

 

Direcciòn del E-mail *

Número de teléfono

 

Department *

Nombre de la Organizaciòn *

 

Country or Region *

Observaciones

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Korean - KR (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.