Guanabenz

Synonyms: GBZ, GA, Wytensin, Wy-8678,BR-750

Guanabenz (GBZ, GA, Wytensin, Wy-8678,BR-750) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.

Guanabenz Chemical Structure

Guanabenz Chemical Structure

CAS No. 5051-62-7

Purity & Quality Control

Batch: S448101 Ethanol]15 mg/mL]false]DMSO]12 mg/mL]false]Water]Insoluble]false Purity: 99.60%
99.60

Guanabenz Related Products

Biological Activity

Description Guanabenz (GBZ, GA, Wytensin, Wy-8678,BR-750) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.
Targets
α2 adrenergic receptor [1]
In vitro
In vitro

Interleukin-6 (IL6), colony stimulating factor 2 (Csf2), and cyclooxygenase-2 (Cox2) are downregulated by guanabenz-driven phosphorylation of eukaryotic translation initiation factor 2α (eIF2α). Although expression of IL1β and Tumor Necrosis Factor-α (TNFα) was suppressed by guanabenz, their downregulation was not directly mediated by eIF2α signaling.[2]

Cell Research Cell lines RAW264.7 macrophages, primary macrophages, Jurkat T lymphocytes and HMC-1.1 mast cells
Concentrations 5, 10, and 20 µM
Incubation Time 2 days
Method

RAW264.7 macrophages and primary macrophages were cultured in αMEM with 10% FBS and antibiotics. Mouse bone marrow cells were grown with 10 ng/mL macrophage colony-stimulating factor for three days, and the surface-attached cells were used as primary macrophages. Jurkat T lymphocytes and HMC-1.1 mast cells were cultured in RPMI 1640 and IMDM with 1-thioglycerol, respectively. RAW264.7 cells and primary macrophages were activated by 0.1 or 1 µg/mL lipopolysaccharide (LPS), while Jurkat cells and HMC-1.1 cells were activated by 100 nM phorbol myristate acetate (PMA) and 1 µM ionomycin. Of note, the MTT assay was conducted by RAW264.7 cells for evaluating cytotoxicity.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04596670 Recruiting
Cancer
Peking University Cancer Hospital & Institute|Peking University Health Science Center
September 20 2024 Early Phase 1
NCT06160271 Not yet recruiting
Non-alcoholic Steatohepatitis
Central Hospital Nancy France
September 1 2024 Phase 2
NCT06376253 Not yet recruiting
Ovarian Cancer|Lung Cancer
Novartis Pharmaceuticals|Novartis
September 6 2024 Phase 1
NCT05170048 Not yet recruiting
Non-Exudative (Dry) Age-related Macular Degeneration (dAMD)
Evergreen Therapeutics Inc.
September 2024 Phase 2
NCT06369831 Not yet recruiting
Metastatic Breast Cancer
ABSCINT NV/SA
August 2024 Phase 2
NCT04495959 Not yet recruiting
Prostatic Cancer
British Columbia Cancer Agency
August 2024 --

Chemical Information & Solubility

Molecular Weight 231.08 Formula
C8H8Cl2N4
CAS No. 5051-62-7 SDF --
Smiles NC(=N)N\N=C\C1=C(Cl)C=CC=C1Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

Ethanol : 15 mg/mL

DMSO : 12 mg/mL ( (51.93 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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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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