Moxonidine hydrochloride
Based on 1 Customer Validation
Moxonidine (BDF5895) hydrochloride is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine hydrochloride activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine hydrochloride reduces atherosclerotic lesions and lowers blood pressure. Moxonidine hydrochloride can be used in the study of hypertension, heart failure, and atherosclerosis.
For research use only. We do not sell to patients.
- Purity: 99.83%
- CAS No.: 75536-04-8
- Formula: C9H13Cl2N5O
- Molecular Weight:278.14
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Biological Activity
Moxonidine (10 μM; 48 h) hydrochloride prevents the mild reduction in cardiomyocyte viability/mitochondrial activity induced by IL-1β and TNF-α[1].
Moxonidine (10 μM; 2 h) hydrochloride increases uptake of oxidised low-density lipoprotein in cultured vascular smooth muscle cells via α2 Adrenoceptors[2].
Moxonidine (30 μM) hydrochloride inhibits voltage-dependent N-type Ca2+ current by activating imidazoline I1 receptors in rat superior cervical ganglion neurons[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Moxonidine (100-1000 μg/kg; i.v.) hydrochloride causes dose-dependent hypotension and bradycardia in conscious wild-type mice[4].
Moxonidine (3-6 mg/kg/day; subcutaneous implantation via osmotic minipumps; 21 days) hydrochloride dose-dependently suppresses myocardial infarction-induced sympathetic activation, and the high dose normalizes ventricular weight-body weight ratio and interstitial collagen in rats with myocardial infarction [5].
Moxonidine (20-80 nmol; intracerebroventricular injection into the fourth ventricle) hydrochloride dose-dependently lowers mean arterial pressure, heart rate and sympathetic outflow in conscious spontaneously hypertensive rats, with stronger effects than when injected into the lateral ventricle[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 75536-04-8
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Appearance Solid
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Molecular Weight 278.14
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Formula C9H13Cl2N5O
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Color White to off-white
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SMILES
CC1=NC(OC)=C(C(Cl)=N1)NC2=NCCN2.[H]Cl
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Synonyms
BDF5895 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
H2O : ≥ 100 mg/mL (359.53 mM)
DMSO : 100 mg/mL (359.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.99 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (563 KB)
- English - EN (563 KB)
- Français - FR (563 KB)
- Deutsch - DE (563 KB)
- Norwegian - NO (563 KB)
- Español - ES (563 KB)
- Swedish - SV (563 KB)
- Italian - IT (563 KB)
- Korean - KR (563 KB)
- Portuguese - PT (563 KB)
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Handling Instructions (2659 KB)
References
[1]. Aceros H, et al. Moxonidine modulates cytokine signalling and effects on cardiac cell viability. Eur J Pharmacol. 2014 Oct 5;740:168-82. [Content Brief]
[2]. Wang Y, et al. Moxonidine Increases Uptake of Oxidised Low-Density Lipoprotein in Cultured Vascular Smooth Muscle Cells and Inhibits Atherosclerosis in Apolipoprotein E-Deficient Mice. Int J Mol Sci. 2023 Feb 14;24(4):3857. [Content Brief]
[3]. Kim YH, et al. Modulation of N-type Ca²⁺ currents by moxonidine via imidazoline I₁ receptor activation in rat superior cervical ganglion neurons. Biochem Biophys Res Commun. 2011 Jun 17;409(4):645-50. [Content Brief]
[4]. Zhu QM, et al. Cardiovascular effects of rilmenidine, moxonidine and clonidine in conscious wild-type and D79N alpha2A-adrenoceptor transgenic mice. Br J Pharmacol. 1999 Mar;126(6):1522-30. [Content Brief]
[5]. Van Kerckhoven R, et al. Chronic administration of moxonidine suppresses sympathetic activation in a rat heart failure model. Eur J Pharmacol. 2000 May 26;397(1):113-20. [Content Brief]
[6]. Nurminen ML, et al. Effect of moxonidine on blood pressure and sympathetic tone in conscious spontaneously hypertensive rats. Eur J Pharmacol. 1998 Nov 27;362(1):61-7. [Content Brief]
[7]. Tsutsui H, et al. Moxonidine prevents ischemia/reperfusion-induced renal injury in rats. Eur J Pharmacol. 2009 Jan 28;603(1-3):73-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.5953 mL | 17.9766 mL | 35.9531 mL | 89.8828 mL |
| 5 mM | 0.7191 mL | 3.5953 mL | 7.1906 mL | 17.9766 mL | |
| 10 mM | 0.3595 mL | 1.7977 mL | 3.5953 mL | 8.9883 mL | |
| 15 mM | 0.2397 mL | 1.1984 mL | 2.3969 mL | 5.9922 mL | |
| 20 mM | 0.1798 mL | 0.8988 mL | 1.7977 mL | 4.4941 mL | |
| 25 mM | 0.1438 mL | 0.7191 mL | 1.4381 mL | 3.5953 mL | |
| 30 mM | 0.1198 mL | 0.5992 mL | 1.1984 mL | 2.9961 mL | |
| 40 mM | 0.0899 mL | 0.4494 mL | 0.8988 mL | 2.2471 mL | |
| 50 mM | 0.0719 mL | 0.3595 mL | 0.7191 mL | 1.7977 mL | |
| 60 mM | 0.0599 mL | 0.2996 mL | 0.5992 mL | 1.4980 mL | |
| 80 mM | 0.0449 mL | 0.2247 mL | 0.4494 mL | 1.1235 mL | |
| 100 mM | 0.0360 mL | 0.1798 mL | 0.3595 mL | 0.8988 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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