| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| ln Vivo |
Guanadrine has low nervous system toxicity in rats and dogs (15–400 mg/kg daily, 6-52 weeks; oral gavage) [1].
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|---|---|
| Animal Protocol |
Animal/Disease Models: Rats, dogs [1]
Doses: 15-400 mg/kg Route of Administration: po (oral gavage); daily; 6-52 weeks Experimental Results: The weight of the prostate and adrenal glands in rats increased slightly, while the weight of the kidneys diminished. Dogs' weight gain diminished in a dose-dependent manner, but liver function was normal. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorbed rapidly and readily from the gastrointestinal tract. Metabolism/Metabolites: Primarily metabolized in the liver. Biological Half-Life: 10 hours. |
| Toxicity/Toxicokinetics |
Low protein binding, approximately 20%
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| References | |
| Additional Infomation |
Guanadrel is a spiroacetal formed by the condensation of the ketone group of cyclohexanone with the hydroxyl group of 1-(2,3-dihydroxypropyl)guanidine. It is a postganglionic adrenergic blocker formerly used to treat hypertension (usually in sulfate form), but has now been superseded by other medications less likely to cause orthostatic hypotension (vertigo upon standing or stretching). Guanadrel has both antihypertensive and adrenergic antagonistic effects. It belongs to the guanidine family and is also a spiroacetal. It is the conjugate base of Guanadrel (1+). Guanadrel is an antihypertensive and postganglionic adrenergic blocker. See also: Guanadrel sulfate (note moved to). Drug Indications For the treatment and control of hypertension. Mechanism of Action Guanadrel is an adrenergic neuron inhibitor that slowly displaces norepinephrine from nerve endings. It blocks the release of norepinephrine caused by sympathetic nerve stimulation, thereby reducing vasoconstriction in small arteries, especially the reflexive increase in sympathetic tone caused by changes in body position.
Pharmacodynamics High blood pressure increases the burden on the heart and arteries. If it persists for a long time, the heart and arteries may not function properly. High blood pressure can damage blood vessels in the brain, heart, and kidneys, leading to stroke, heart failure, or kidney failure. High blood pressure also increases the risk of heart attack. If blood pressure is controlled, the chances of these problems occurring are reduced. Guanazore works by controlling nerve impulses on specific neural pathways. Therefore, it can relax blood vessels, making it easier for blood to flow. This helps lower blood pressure. |
| Molecular Formula |
C10H19N3O2
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|---|---|
| Molecular Weight |
213.27676
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| Exact Mass |
213.148
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| CAS # |
40580-59-4
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| Related CAS # |
22195-34-2 (sulfate[2:1])
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| PubChem CID |
38521
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| Appearance |
Colorless to light yellow ointment
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| Density |
1.39g/cm3
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| Boiling Point |
387.9ºC at 760 mmHg
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| Melting Point |
213.5-215ºC
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| Flash Point |
188.4ºC
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| Index of Refraction |
1.618
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| LogP |
1.736
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
245
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N/C(=N/CC1COC2(CCCCC2)O1)/N
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| InChi Key |
HPBNRIOWIXYZFK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H19N3O2/c11-9(12)13-6-8-7-14-10(15-8)4-2-1-3-5-10/h8H,1-7H2,(H4,11,12,13)
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| Chemical Name |
2-(1,4-dioxaspiro[4.5]decan-3-ylmethyl)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 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 : ~50 mg/mL (~234.43 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.72 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 (11.72 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 (11.72 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 | 4.6887 mL | 23.4434 mL | 46.8867 mL | |
| 5 mM | 0.9377 mL | 4.6887 mL | 9.3773 mL | |
| 10 mM | 0.4689 mL | 2.3443 mL | 4.6887 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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