Guanabenz Acetate

Catalog No.S4065 Batch:S406502

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Technical Data

Formula

C8H8Cl2N4.C2H4O2
Molecular Weight 291.13 CAS No. 23256-50-0
Solubility (25°C)* In vitro DMSO 15 mg/mL (51.52 mM)
Ethanol 15 mg/mL (51.52 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
4%DMSO 30%PEG300 66%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 300 μL of PEG 300, mix evenly to clarify it; then continue to add 660 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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 Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.
Targets
α2a-adrenergic receptor [1] α2b-adrenergic receptor [1] α2c-adrenergic receptor [1]
8.25(pEC50) 7.01(pEC50) <5(pEC50)
In vitro Guanabenz at a concentration of 30 μM causes a time-dependent loss of nNOS-activity, which is present in cytosol prepared from rat nNOS transfected HEK 293 cells, with a Ki of 1 μM. Guanabenz can induce a concentration-dependent loss of nNOS activity. Within the first 3 h of treatment, 50 μM Guanabenz decreases the accumulation of nitrite and nitrate by approximately 75% in cells. Treatment of HEK 293 cells for 24 h with Guanabenz (100 μM) causes an approximately 35% decrease in the amount of immunodetectable nNOS protein. Guanabenz enhances proteolysis of the protein with the half-life decreasing by one-half from 20 to 10 h. [2] Guanabenz is active against [ PSI+] prion in the yeast-based assay independent of its agonist activity on α2-adrenergic receptors. Guanabenz (10 μM) promote complete PrPSc clearance in mammalian MovS6 cell-based assay. [3]
In vivo Guanabenz injected i.v. in doses of 0.1 mg/kg causes an initial increase in blood pressure followed by a prolonged fall and a decrease in cardiac output, contractile force and heart rate in anesthetized dogs, which requires the presence of sympathetic tone. Guanabenz inhibits pressor responses to various procedures which initiate general sympathetic discharge. Guanabenz also antagonizes responses to sympathetic nerve stimulation. [4] Guanabenz injected at doses of 0.5 mg/kg and above lowers blood pressure and heart rate in unanesthetized hypertensive rats and dogs. [5]

Protocol (from reference)

Selleck's Guanabenz Acetate has been cited by 2 publications

Androgen Signaling Regulates SARS-CoV-2 Receptor Levels and Is Associated with Severe COVID-19 Symptoms in Men [ Cell Stem Cell, 2020, 27(6):876-889.e12] PubMed: 33232663
Targeting Super-Enhancer-Driven Oncogenic Transcription by CDK7 Inhibition in Anaplastic Thyroid Carcinoma. [ Thyroid, 2019, 29(6):809-823] PubMed: 30924726

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.