Home Endocrinology & Hormones Adrenergic Receptor agonist Guanabenz For research use only.

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: 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

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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
NCT04495959 Not yet recruiting Prostatic Cancer British Columbia Cancer Agency August 2024 --
NCT05739942 Not yet recruiting Newly Diagnosed and Recurrent Glioblastoma Novartis Pharmaceuticals|Novartis April 1 2024 Phase 1

Chemical lnformation & 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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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.

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