| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Target is the α2-adrenergic receptor, with selectivity for α2 over α1 subtypes; guanabenz binds α2B and α2C receptors with pKi values around 6.8 and activates Gi/o-mediated signaling, reducing sympathetic tone and peripheral vascular resistance, and it also modulates endoplasmic reticulum stress responses.
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|---|---|
| ln Vitro |
Guanabenz is a selective α2-adrenergic agonist that reduces sympathetic outflow and lowers blood pressure; in vitro, it activates α2-adrenergic receptors with pKi values in the 6–7 range, inhibits adenylyl cyclase via Gi/o coupling, and shows neuroprotective activity in cellular models of ER stress and protein aggregation.
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| ln Vivo |
In vivo, guanabenz produces pronounced hypotension by reducing peripheral vascular resistance, heart rate, and cardiac output; it is effective in hypertensive animal models after oral administration, and it shows neuroprotective effects in models of prion disease and other neurodegenerative conditions through ER stress modulation.
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| Enzyme Assay |
α2-Adrenergic receptor binding is measured using membranes from tissues or cells expressing α2A, α2B, or α2C receptors and a radioligand such as [3H]clonidine or [3H]RX821002; graded guanabenz concentrations displace the radioligand, and Ki values are calculated; functional agonism is confirmed by GTPγS binding or cAMP inhibition assays.
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| Cell Assay |
Cells expressing α2-adrenergic receptors are treated with guanabenz, and GTPγS binding, cAMP accumulation, or ERK phosphorylation are measured; neuroprotective activity is assessed in neuronal cell lines under ER stress or proteotoxic stress, with cell viability measured by metabolic assays and ER stress markers by Western blotting.
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| Animal Protocol |
Hypertensive rats or mice receive guanabenz by oral or intraperitoneal administration at doses selected from pharmacokinetic studies; blood pressure and heart rate are monitored by telemetry or tail-cuff, plasma catecholamines are measured by HPLC, and brain and plasma drug concentrations are quantified to correlate α2 receptor occupancy with hemodynamic effects.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Approximately 75% is absorbed via the gastrointestinal tract. Metabolism/Metabolites Hepatic metabolism. Known metabolites of guanethidine in humans include guanethoxabine. Biological Half-Life 6 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation Since there is currently no information regarding the use of guanethidine during lactation, it is recommended to prioritize other medications, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. Protein Binding Rate 90% |
| References |
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| Additional Infomation |
Guanabenz is a dichlorobenzene compound. Guanabenz is a centrally acting alpha-2-adrenergic agonist. Its mechanism of action is as an alpha-2-adrenergic agonist. It is a selective alpha-2-adrenergic agonist used as an antihypertensive drug. See also: Guanabenz acetate (in salt form). Drug Indications For the treatment of hypertension. FDA label. Mechanism of Action The antihypertensive effect of Guanabenz is thought to be due to central alpha-adrenergic stimulation, leading to a reduction in sympathetic nerve output to the heart, kidneys, and peripheral blood vessels, while lowering systolic and diastolic blood pressure and slightly slowing the pulse rate. Long-term use of Guanabenz also leads to a decrease in peripheral vascular resistance.
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| Molecular Formula |
C8H8CL2N4
|
|---|---|
| Exact Mass |
230.013
|
| CAS # |
60329-03-5
|
| Related CAS # |
Guanabenz hydrochloride;23113-43-1;Guanabenz;5051-62-7
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| PubChem CID |
5702063
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| Appearance |
Typically exists as solid at room temperature
|
| Melting Point |
225-227
|
| LogP |
3.001
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
14
|
| Complexity |
228
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N/C(=N\N=C\C1=C(Cl)C=CC=C1Cl)/N
|
| InChi Key |
WDZVGELJXXEGPV-YIXHJXPBSA-N
|
| InChi Code |
InChI=1S/C8H8Cl2N4/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12/h1-4H,(H4,11,12,14)/b13-4+
|
| Chemical Name |
2-[(E)-(2,6-dichlorophenyl)methylideneamino]guanidine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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