| Field | Specification |
|---|---|
| Alternative names | BDF5895 hydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C9H13Cl2N5O |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Moxonidine hydrochloride, also known as BDF5895 hydrochloride, is an orally active agonist of the imidazoline type 1 receptor (I1-R). It activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake, and it reduces atherosclerotic lesions and lowers blood pressure. It can be used in the study of hypertension, heart failure, and atherosclerosis[1][2][3][4][5][6][7]. It is supplied as a white to off-white solid (C9H13Cl2N5O, MW 278.14) at 99.83% purity.
Physical & Chemical Properties
| CAS Number | 75536-04-8 |
|---|---|
| Molecular Formula | C9H13Cl2N5O |
| Molecular Weight | 278.14 g/mol |
| Purity | 99.83% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | CC1=NC(OC)=C(C(Cl)=N1)NC2=NCCN2.[H]Cl |
| Signaling Pathway | Neuronal Signaling; GPCR/G Protein; Metabolic Enzyme/Protease |
| Solubility | In Vitro: H2O: ≥ 100 mg/mL (359.53 mM) DMSO: 100 mg/mL (359.53 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) * "≥" means soluble, but saturation unknown. |
| 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). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| H2O | ≥ 100 mg/mL (359.53 mM) | — |
| DMSO | 100 mg/mL (359.53 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture and light; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (8.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (8.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (8.99 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Moxonidine hydrochloride (10 μM; 48 h) prevents the mild decrease in cardiomyocyte viability/mitochondrial activity caused by IL-1β and TNF-α[1]. In cultured vascular smooth muscle cells, Moxonidine hydrochloride (10 μM; 2 h) raises uptake of oxidised low-density lipoprotein via α2 Adrenoceptors[2]. Moxonidine hydrochloride (30 μM) blocks voltage-dependent N-type Ca2+ current in rat superior cervical ganglion neurons by activating imidazoline I1 receptors[3].
In Vivo
In ApoE-/- mice infused with Angiotensin II, Moxonidine hydrochloride (18 mg/kg/day; p.o.; via drinking water) reduces the formation of atherosclerosis in the aortic arch and in the left common carotid artery, together with increased plasma lipid hydroperoxide levels[2]. Moxonidine hydrochloride (100-1000 μg/kg; i.v.) produces dose-dependent hypotension and bradycardia in conscious wild-type mice[4]. In rats with myocardial infarction, Moxonidine hydrochloride (3-6 mg/kg/day; subcutaneous implantation via osmotic minipumps; 21 days) suppresses sympathetic activation induced by myocardial infarction in a dose-dependent manner, while the high dose brings ventricular weight-body weight ratio and interstitial collagen back to normal[5]. In conscious spontaneously hypertensive rats, Moxonidine hydrochloride (20-80 nmol; intracerebroventricular injection into the fourth ventricle) lowers mean arterial pressure, heart rate and sympathetic outflow dose-dependently, with stronger effects than injection into the lateral ventricle[6].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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