| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Guanabenz HCl targets alpha-2 adrenergic receptors (α2-adrenoceptors) in the brainstem. It is a centrally acting α2-adrenergic receptor agonist with effective concentrations of 10-100 nM. By activating these receptors, it decreases sympathetic outflow from the central nervous system, leading to reduced peripheral vascular resistance and lowered blood pressure. It also induces ER stress and triggers the unfolded protein response (UPR).
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| ln Vitro |
Cell viability is not affected by treating guanidine hydrochloride (0.5-50 μM) at escalating concentrations for a full day [1]. UPR targets were not impacted by guanidine hydrochloride alone (0.5–50 μM, 24 h), neither at the mRNA or protein levels nor the phosphorylation state of eIF2a. Furthermore, neither GADD34 nor the constitutively active version of CReP are induced by guanabenz[1]. In newborn rat cardiomyocytes, guanidine hydrochloride alone (0.5–50 μM, 24 hours) does not cause endoplasmic reticulum stress [1].
In vitro, Guanabenz HCl acts as an α2-adrenergic receptor agonist with effective concentrations of 10-100 nM. It induces endoplasmic reticulum (ER) stress and triggers the unfolded protein response (UPR). It has antiparasitic activity. It interferes with ER stress signaling and has protective effects in cardiac myocytes. These in vitro activities demonstrate its potential for studying adrenergic signaling, ER stress, and cardioprotection. |
| ln Vivo |
Brain cyst burden is consistently decreased by guanidine hydrochloride (5 mg/kg/day; intraperitoneally; for 3 weeks) [2]. In mice with latent Toxoplasma gondii infection, guanidine hydrochloride (5 mg/kg/d intraperitoneal injection, orally; 10 mg/kg/d gavage, for 3 weeks) can reverse hyperactivity [2]. In debuffered cats, guanidine hydrochloride (100 and 320 μg/kg and 1 mg/kg, intravenously given for 5 minutes at 40-minute intervals) lowers blood pressure, heart rate, and sympathetic outflow [3].
In vivo, Guanabenz HCl is used as an antihypertensive agent. It is orally active and lowers blood pressure by stimulating alpha-2 adrenergic receptors in the brainstem. It has been used clinically for the management of hypertension. It also has antiparasitic activity. In cardiac myocytes, it has protective effects. |
| Enzyme Assay |
In vitro receptor binding assays are used to characterize Guanabenz HCl's affinity for α2-adrenergic receptors. Membrane preparations from cells expressing the receptors are incubated with radiolabeled ligands and varying concentrations of the compound. Bound radioactivity is measured, and binding parameters are calculated. Functional assays measure downstream signaling including cAMP inhibition.
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| Cell Assay |
Cell viability assay [1]
Cell Types: Newborn rat cardiomyocytes (NRCM) Tested Concentrations: 0.5-50 μM Incubation Duration: 24 h Experimental Results: Does not affect cell survival. Western Blot Analysis [1] Cell Types: Neonatal rat cardiomyocytes (NRCM) Tested Concentrations: 0.5-50 μM Incubation Duration: 24 hrs (hours) Experimental Results: The levels of UPR target proteins increased in a concentration-dependent manner in the low group. RT-PCR[1] Cell Types: Neonatal rat cardiomyocytes (NRCM) Tested Concentrations: 0.5-50 μM Incubation Duration: 24 hrs (hours) Experimental Results: Does not affect the levels of UPR targets. Cell-based assays for Guanabenz HCl are conducted in cells expressing α2-adrenergic receptors. Cells are treated with the compound at concentrations of 10-100 nM, and effects on cAMP levels, ER stress markers, and cell viability are assessed. ER stress is evaluated by measuring markers such as CHOP, BiP, and ATF4. |
| Animal Protocol |
Animal/Disease Models: BALB/cJ mice [2]
Doses: 5 mg/kg Doses: 5 mg/kg/day; ip; for 3 weeks Experimental Results: Latent brain cysts were diminished in both male and female BALB/cJ mice . Animal/Disease Models: BALB/cJ mice[2] Doses: 5 mg/kg; 10 mg/kg Route of Administration: 5 mg/kg/d, intraperitoneal (ip) injection, oral administration; 10 mg/kg/d, gavage; last for 3 weeks Experimental Results: Reversal of parasite-induced hyperactivity to near baseline levels. Animal/Disease Models: Cat [3] Doses: 100 and 320 μg/kg and 1 mg/kg Route of Administration: 100 and 320 μg/kg and 1 mg/kg, intravenously (iv) (iv)(iv) for 5 minutes at 40 minute intervals Experimental Results: Rejection of blood pressure and Neural activity is evident. In vivo animal experiments with Guanabenz HCl are conducted in hypertensive animal models. The compound is administered orally, and blood pressure is measured. Antiparasitic activity is evaluated in parasite infection models. Cardioprotective effects are assessed in models of cardiac injury. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Guanabenz HCl include oral activity and good oral bioavailability. The compound is absorbed after oral administration and crosses the blood-brain barrier to reach its central targets. It undergoes hepatic metabolism. Specific PK parameters such as half-life and Cmax have been reported in clinical literature. Storage: 2-8°C, protected from light, desiccated.
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| Toxicity/Toxicokinetics |
Guanabenz HCl has been used clinically as an antihypertensive agent. Common adverse effects include drowsiness, dry mouth, dizziness, and weakness. It is for research use and for approved clinical applications; not for over-the-counter use. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Christiane Neuber, et al. Guanabenz interferes with ER stress and exerts protective effects in cardiac myocytes. PLoS One. 2014 Jun 3;9(6):e98893.
[2]. Jennifer Martynowicz, et al. Guanabenz Reverses a Key Behavioral Change Caused by Latent Toxoplasmosis in Mice by Reducing Neuroinflammation. mBio. 2019 Apr 30;10(2):e00381-19. [3]. T Baum, et al. Studies on the centrally mediated hypotensive activity of guanabenz. Eur J Pharmacol. 1976 May;37(1):31-44. |
| Additional Infomation |
Guanabenz HCl has CAS number 23113-43-1, molecular formula C8H9Cl3N4, and molecular weight 267.54. Synonyms: Wytensin. It is an orally active α-2 adrenoceptor agonist with antihypertensive and antiparasitic activity. It works by stimulating alpha-2 adrenergic receptors in the brainstem. Purity: ≥98%. Storage: 2-8°C, protected from light, desiccated. Not for over-the-counter use; for research and approved clinical applications.
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| Molecular Formula |
C8H8N4CL2.HCL
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| Molecular Weight |
267.54286
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| Exact Mass |
265.989
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| CAS # |
23113-43-1
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| Related CAS # |
Guanabenz;5051-62-7;(E)-Guanabenz;60329-03-5
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| PubChem CID |
9577025
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| Appearance |
White to off-white solid powder
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| Boiling Point |
405.7ºC at 760mmHg
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| Flash Point |
199.1ºC
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| Vapour Pressure |
8.63E-07mmHg at 25°C
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| LogP |
3.803
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
228
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.N/C(=N/N=C/C1C(Cl)=CC=CC=1Cl)/N
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| InChi Key |
UNWWUUPHJRAOMZ-GAYQJXMFSA-N
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| InChi Code |
InChI=1S/C8H8Cl2N4.ClH/c9-6-2-1-3-7(10)5(6)4-13-14-8(11)12;/h1-4H,(H4,11,12,14);1H/b13-4+;
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| Chemical Name |
2-[(E)-(2,6-dichlorophenyl)methylideneamino]guanidine;hydrochloride
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
DMSO : ~100 mg/mL (~373.78 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7378 mL | 18.6888 mL | 37.3776 mL | |
| 5 mM | 0.7476 mL | 3.7378 mL | 7.4755 mL | |
| 10 mM | 0.3738 mL | 1.8689 mL | 3.7378 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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