Guanfacine Hydrochloride

Catalog No.S4693 Synonyms: Guanfacine, Tenex, Intuniv

For research use only.

Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.

Guanfacine Hydrochloride Chemical Structure

CAS No. 29110-48-3

Purity & Quality Control

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Biological Activity

Description Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.
Targets
α2A-adrenoceptor [1]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: LLC-PK1 and LLC-PK1/MDR1 cells 
  • Concentrations: 5 μM
  • Incubation Time: 1 h
  • Method:

    Cells (1 mL) are seeded into 24-well plates at a density of 1 × 105 cells/mL. Culture medium is replaced every two days until cells reached confluence. To investigate the potential influence of P-gp on guanfacine transport, intracellular accumulation of guanfacine is measured in LLC-PK1/MDR1 cells and P-gp-negative LLC-PK1 cells. Rhodamine6G, a well-known P-gp substrate, is included as a positive control. After cells reach confluence, the culture medium is replaced by transport buffer for a 30-minute preincubation at 37°C. Transport buffer is then removed and the test compounds (5 μM rhodamine6G, 5 μM guanfacine, or 50 μM guanfacine) are added, and an additional 60-minute incubation period commenced. Next, the solutions are discarded, and the cells are washed three times with ice-cold Dulbecco’s phosphate-buffered saline and solubilized with 1% Triton X-100. Intracellular accumulation of rhodamine6G is measured using a fluorescent microplate reader with a 530 nm excitation and a 580 nm emission wavelength, which is a well established method. Cellular retention of guanfacine is analyzed by the high-performance liquid chromatographic assay described below. The concentrations of rhodamine6G and guanfacine are calculated from their respective standard curves, and standardized with the cellular protein content determined by a Pierce bicinchoninic acid protein kit.

Animal Research:

[1]

  • Animal Models: Rats
  • Dosages: 0.075, 0.15, 0.3, and 0.6 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 282.55
Formula

C9H9Cl2N3O.HCl

CAS No. 29110-48-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C(=C1)Cl)CC(=O)N=C(N)N)Cl.Cl

In vivo Formulation Calculator (Clear solution)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04866030 Completed -- Attention Deficit Hyperactivity Disorder (ADHD) Shire|Takeda March 11 2019 --
NCT01904526 Completed Drug: Guanfacine Smoking Yale University|National Institute on Drug Abuse (NIDA) July 2013 Phase 2
NCT00919867 Completed Drug: SPD503|Drug: VYVANSE|Drug: SPD503 and VYVANSE Healthy Shire|Takeda June 24 2009 Phase 1
NCT00901576 Completed Drug: SPD503|Drug: Concerta|Drug: SPD503 + Concerta Healthy Shire|Takeda May 18 2009 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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