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Guanethidine Sulfate

Catalog No.GC15934

Antihypertensive compound

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Guanethidine Sulfate Chemical Structure

Cas No.: 645-43-2

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1g
$60.00
In stock
5g
$178.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

the electrically stimulated mouse vas deferens

Preparation method

This compound is soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

3 μM

Applications

In the electrically stimulated mouse vas deferens, Guanethidine sulfate inhibited twitching by 95%±3% in 15 min, but this effect was only partially reversed after 1 h of washing (33%±12% of control).

Animal experiment [1]:

Animal models

Myocardial infarction (MI) rat model

Dosage form

low-dose [LG], 1 mg/kg/day; medium-dose, 3 mg/kg/day; high-dose, 10 mg/kg/day; administered via an osmotic mini-pump for 4 weeks

Application

In myocardial infarction (MI) rats, LG suppressed left ventricular (LV) dilation (9.2±0.9 mm vs.11.0±0.8 mm) and improved LV fractional shortening (25.0±4.5% vs. 16.4±4.7%) in association with a reduction of plasma NE levels (520±250 pg/ml vs.1,000±570 pg/ml). Low-dose guanethidine reduced 24-h (6%) and 28-day mortality (6%). High-dose guanethidine also reduced 24-h mortality (12%) but increased 28-day mortality (91%).

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Joyce PI1,Rizzi D,Caló G,Rowbotham DJ,Lambert DG. The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens.Anesth Analg.2002 Nov;95(5):1339-43, table of contents.

[2]. Igawa A1, Nozawa T, Fujii N, et al. Long-term treatment with low-dose, but not high-dose, guanethidine improves ventricular function and survival of rats with heart failure after myocardial infarction. J Am Coll Cardiol. 2003 Aug 6;42(3):541-8.

Background

Guanethidine Sulfate is an anti-hypertensive drug involved in reducing the release of catecholamines such as norepinephrine [1].

In vitro: Guanethidine (0.1 and 1 μM) decreased S-I efflux but increased resting efflux in a concentration dependent manner[1].On the electrically stimulated mouse vas deferens, Guanethidine (3 μM) treatment inhibited twitching by 95% ± 3% in 15 min, but this effect was only partially reversed after 1 h of washing (33% ± 12% of control). When guanethidine were used in combination with prilocaine, a reversal of 80% ± 13% (at 1 h) was observed. When co-incubated with guanethidine (3 μM), the twitch was reduced to 24% ± 4% of control and was reversed to 77% ± 7% after 1 h. The reversal produced by the combination was significantly more intense (P < 0.05) when compared with guanethidine alone. Local anesthetics reduced the sympatholytic actions of guanethidine, and this could explain the variable efficacy of guanethidine in the treatment of complex regional pain syndrome [2].

References:
[1]. Fabiani ME1,Story DF. Inhibition of sympathetic noradrenergic transmission by guanabenz and guanethidine in rat isolated mesenteric artery: involvement of neuronal potassium channels.Pharmacol Res.1996 Mar;33(3):171-80.
[2]. Joyce PI1,Rizzi D,Caló G,Rowbotham DJ,Lambert DG. The effect of guanethidine and local anesthetics on the electrically stimulated mouse vas deferens.Anesth Analg.2002 Nov;95(5):1339-43, table of contents.

Chemical Properties

Cas No. 645-43-2 SDF
Chemical Name 2-[2-(azocan-1-yl)ethyl]guanidine;sulfuric acid
Canonical SMILES C1CCCN(CCC1)CCN=C(N)N.C1CCCN(CCC1)CCN=C(N)N.OS(=O)(=O)O
Formula C10H24N4O4S M.Wt 296.39
Solubility ≥ 159.4mg/mL in Water Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.3739 mL 16.8697 mL 33.7393 mL
5 mM 0.6748 mL 3.3739 mL 6.7479 mL
10 mM 0.3374 mL 1.687 mL 3.3739 mL
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In vivo Formulation Calculator (Clear solution)

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

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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.)

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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.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 21 reference(s) in Google Scholar.)

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