>>Signaling Pathways>> Others>> Imidazoline Receptors>>Moxonidine

Moxonidine (Synonyms: LY326869)

Catalog No.GC12629

An imidazoline I1 and α2A-adrenergic receptor agonist

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Moxonidine Chemical Structure

Cas No.: 75438-57-2

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$36.00
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10mg
US$48.00
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50mg
US$144.00
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Sample solution is provided at 25 µL, 10mM.

Description of Moxonidine

Moxonidine is an agonist of I1-imidazoline receptor with EC50 value of 1.3µM [1].

Moxonidine can bind to both I1-imidazoline receptor (I1R) and α2-adrenergic receptor (α2AR). The selectivity of moxonidine for I1R is 33-fold over α2AR. Moxonidine plays its antihypertensive role in the central nervous system. It has a central site of action. It is shown no effect in pithed rats and in cats following spinal cord transaction. Moxonidine also reduces sympathetic outflow and lowers peripheral vascular resistence [1, 2].

Besides the antihypertensive efficacy, Moxonidine is reported to have effects on gastric secretion and gastric mucosal injury in rats. It significantly reduces basal gastric acid secretion when given doses of 0.1 (63% inhibition) and 1.0 (65% inhibition) mg/kg. Even 0.01mg/kg moxonidine can reduce the gastric mucosal injury induced by ethanol [3].

References:
[1] George OK, Gonzalez RR Jr, Edwards LP. Moxonidine, an antihypertensive agent, is permissive to alpha1-adrenergic receptor pathway in the rat-tail artery. J Cardiovasc Pharmacol. 2004 Feb;43(2):306-11.
[2] Morris ST, Reid JL. Moxonidine: a review. J Hum Hypertens. 1997 Oct;11(10):629-35.
[3] Glavin GB, Smyth DD. Effects of the selective I1 imidazoline receptor agonist, moxonidine, on gastric secretion and gastric mucosal injury in rats. Br J Pharmacol. 1995 Feb;114(4):751-4.

Chemical Properties of Moxonidine

Cas No. 75438-57-2 SDF
Synonyms LY326869
Chemical Name 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methylpyrimidin-5-amine
Canonical SMILES CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC
Formula C9H12ClN5O M.Wt 241.68
Solubility ≥ 11.3 mg/mL in DMSO, ≥ 4.74 mg/mL in EtOH with ultrasonic 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 of Moxonidine

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1 mg 5 mg 10 mg
1 mM 4.1377 mL 20.6885 mL 41.377 mL
5 mM 0.8275 mL 4.1377 mL 8.2754 mL
10 mM 0.4138 mL 2.0689 mL 4.1377 mL
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In vivo Formulation Calculator (Clear solution) of Moxonidine

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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 30 reference(s) in Google Scholar.)

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