| Size | Price | Stock | Qty |
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| 5mg |
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| 25mg |
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Purity: ≥98%
| Targets |
Guanoclor (CAS#: 5001-32-1) binds to non-adrenergic sites in pig kidney membranes (IC₅₀ for inhibition of [³H]idazoxan binding = 10 ± 5 nM).[1]
Guanoclor (CAS#: 5001-32-1) inhibits Na⁺/H⁺ exchange activity with an IC₅₀ of 1 μM.[1] Guanoclor targets the sympathetic nervous system. It acts as a sympatholytic agent, reducing sympathetic outflow from the central nervous system. This leads to decreased peripheral vascular resistance and reduced blood pressure. The compound is a guanidine derivative with antihypertensive properties. |
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| ln Vitro |
Guanoclor (CAS#: 5001-32-1) potently inhibited specific [³H]idazoxan binding to pig kidney membranes in a concentration-dependent manner, with an IC₅₀ value of 10 ± 5 nM (n=3). It was among the most potent imidazolidines tested, slightly more potent than guanabenz (IC₅₀ = 18 ± 5 nM) and guanoxan (IC₅₀ = 20 ± 3 nM).[1]
Guanoclor (CAS#: 5001-32-1) inhibited Na⁺/H⁺ exchange activity with an IC₅₀ of 1 μM, as previously reported (Frelin et al., 1986).[1] Guanoclor reduces blood pressure by decreasing sympathetic nervous system activity. It has been used clinically as an antihypertensive agent. The compound's mechanism involves reducing peripheral vascular resistance through sympathetic inhibition, leading to decreased blood pressure. |
| ln Vivo |
In vivo, Guanoclor was used as an antihypertensive agent for the treatment of hypertension. It reduces blood pressure through its sympatholytic effects. The compound was administered orally and had clinical efficacy in lowering blood pressure.
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| Enzyme Assay |
For [³H]idazoxan binding experiments, crude pig kidney membranes were incubated with 2 nM [³H]idazoxan in a buffer consisting of 2 mM EGTA, 1 mM MgCl₂, and 50 mM Tris-Cl at pH 7.4. The incubation was carried out for 45 minutes at 20°C. Bound and free ligand were separated by rapid vacuum filtration through GF/C filters, and the bound radioactivity was determined by liquid scintillation counting. Non-specific binding was determined in the presence of 10 μM tolazoline or 10 μM guanoxan. In competition experiments, various concentrations of unlabeled compounds (including Guanoclor (CAS#: 5001-32-1)) were tested in duplicate at least 10 concentrations. IC₅₀ values are defined as the concentration required to inhibit specific [³H]idazoxan binding by 50%.[1]
Cell-free assays for Guanoclor are not typically performed as its mechanism of action involves central sympathetic nervous system effects rather than direct receptor binding that can be easily measured in cell-free systems. Receptor binding assays could potentially be developed to assess its interactions with adrenergic receptors. |
| Cell Assay |
Cells expressing adrenergic receptors or neuronal cells could be treated with Guanoclor to assess its effects on sympathetic signaling. However, specific cellular assays for this compound are not well documented in the literature.
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| Animal Protocol |
In vivo animal studies for Guanoclor were historically conducted in rodent and dog models of hypertension. The compound was administered orally or intravenously. Blood pressure and heart rate were measured to assess antihypertensive efficacy.
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| ADME/Pharmacokinetics |
Guanoclor is orally bioavailable. As a small molecule (MW 213.7, formula C8H12ClN5), it is absorbed after oral administration. The compound is metabolized in the liver and excreted primarily by the kidneys. PK parameters have been characterized in historical studies.
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| Toxicity/Toxicokinetics |
Guanoclor has been associated with adverse effects including orthostatic hypotension, dizziness, and fatigue. As a sympatholytic agent, it has potential for sedation and other CNS effects. Standard toxicological assessments were conducted historically to support clinical use.
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| References |
Eur J Pharmacol.1989 Jan 31;160(2):295-8.
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| Additional Infomation |
Guanoclor is a dichlorobenzene.
See also: Guanoclor sulfate (note moved to). Guanoclor (CAS#: 5001-32-1) is an imidazolidine derivative recognized for its antihypertensive properties, traditionally believed to act as a central α₂-adrenoceptor agonist. This study demonstrates that it also binds with high affinity (IC₅₀ = 10 nM) to a novel class of non-adrenergic binding sites in pig kidney membranes. These sites are distinct from α₂-adrenoceptors (yohimbine binding sites), clonidine-preferring sites, the Na⁺/H⁺ exchanger, and the epithelial Na⁺ channel, as [³H]idazoxan binding was not displaced by adrenergic compounds (epinephrine, prazosin, phenylephrine, yohimbine) and amiloride derivatives showed different potency orders.[1] Guanoclor (molecular formula C8H12ClN5, MW 213.7) is an antihypertensive agent that acts as a sympatholytic agent. It is a guanidine derivative that was used clinically for the treatment of hypertension. The compound is also known by the brand name Wytensin. It is intended for research use only. |
| Molecular Formula |
C9H12CL2N4O
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|---|---|
| Molecular Weight |
263.1238
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| Exact Mass |
262.039
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| Elemental Analysis |
C, 41.08; H, 4.60; Cl, 26.95; N, 21.29; O, 6.08
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| CAS # |
5001-32-1
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| PubChem CID |
71835
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| Appearance |
White to off-white solid powder
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| Density |
1.48 g/cm3
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| Boiling Point |
435.1ºC at 760mmHg
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| Flash Point |
216.9ºC
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| Index of Refraction |
1.617
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| LogP |
2.941
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
16
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| Complexity |
226
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C([H])C([H])=C(C=1OC([H])([H])C([H])([H])N([H])/N=C(\N([H])[H])/N([H])[H])Cl
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| InChi Key |
XIHXRRMCNSMUET-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H12Cl2N4O/c10-6-2-1-3-7(11)8(6)16-5-4-14-15-9(12)13/h1-3,14H,4-5H2,(H4,12,13,15)
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| Chemical Name |
2-[2-(2,6-dichlorophenoxy)ethylamino]guanidine
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| Synonyms |
Guanoclor; VATENSOL; 2-(2-(2,6-dichlorophenoxy)ethyl)hydrazine-1-carboximidamide;
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8005 mL | 19.0027 mL | 38.0055 mL | |
| 5 mM | 0.7601 mL | 3.8005 mL | 7.6011 mL | |
| 10 mM | 0.3801 mL | 1.9003 mL | 3.8005 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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