Guanfacine Hydrochloride

Catalog No.S4693 Batch:S469301

Technical Data

Formula	C₉H₉Cl₂N₃O.HCl
Molecular Weight	282.55	CAS No.	29110-48-3
Solubility (25°C)*	In vitro	DMSO	56 mg/mL (198.19 mM)
		Ethanol	56 mg/mL (198.19 mM)
		Water	30 mg/mL (106.17 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[1]}	Animal Models Rats Dosages 0.075, 0.15, 0.3, and 0.6 mg/kg Administration i.p.

Cell Assay:^{^[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 Study:^{^[1]}

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

References

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.