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Guanabenz Adrenergic Receptor agonist

Name: Guanabenz
Brand: Selleck Chemicals
SKU: S4481
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4481

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

Chemical Structure

Molecular Weight: 231.08

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.60

Related Targets	Estrogen/progestogen Receptor GPR Androgen Receptor Glucocorticoid Receptor ACE RAAS Progesterone Receptor Opioid Receptor PGES THR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride L755507 Yohimbine HCl Atipamezole Higenamine hydrochloride Detomidine HCl Naftopidil Demethyl-Coclaurine Buflomedil HCl Fenoterol hydrobromide

Solubility

In vitro
Batch:

Ethanol : 15 mg/mL

DMSO : 12 mg/mL (51.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.600mg/ml (2.60mM)	Taking the 1 mL working solution as an example, add 50 μL of 12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	231.08	Formula	C₈H₈Cl₂N₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	5051-62-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GBZ, GA, Wytensin, Wy-8678,BR-750			Smiles	NC(=N)N\N=C\C1=C(Cl)C=CC=C1Cl

Mechanism of Action

Targets/IC₅₀/Ki	α2 adrenergic receptor
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/6352237/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4881500/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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	--

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