[CAS NO. 75438-57-2]  Moxonidine

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PRODUCTS SPECIFICATIONS [75438-57-2]

Catalog
HY-B0374
Brand
MCE
CAS
75438-57-2

DESCRIPTION [75438-57-2]

Overview

MDLMFCD00865794
Molecular Weight241.68
Molecular FormulaC9H12ClN5O
SMILESCC1=NC(OC)=C(NC2=NCCN2)C(Cl)=N1

For research use only. We do not sell to patients.

Summary

Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent. Target: I1-R Moxonidine is a centrally acting antihypertensive agent. Mixed Nischarin (I1 imidazoline receptor) and α2-AR (adrenergic) agonist; displays 40-fold higher affinity for I1 receptors versus α2-adrenoceptors. Moxonidine reduced stimulated NE overflow (log EC50: -6.15 +/- 0.14). AGN192403, a selective ligand at I1-R, had no influence on the dose-response curve of moxonidine (log EC50: -6.01 +/- 0.25) [1]. The hypotensive and bradycardic actions of moxonidine but not clonidine are mediated through imidazoline receptors and are dependent on intact noradrenergic pathways within the RVLM. Furthermore, the noradrenergic innervation may be associated with a 42 kDa imidazoline receptor protein [2].


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04329806 Italo Biaggioni|National Heart, Lung, and Blood Institute (NHLBI)|Vanderbilt University Medical Center
Obesity-Associated Insulin Resistance
February 23, 2021 Phase 1
NCT04023565 Sergey V. Nedogoda|Volgograd State Medical University
Arterial Hypertension|Metabolic Syndrome
March 11, 2019 Phase 4
NCT01504321 Baker Heart and Diabetes Institute
Polycystic Ovary Syndrome
May 2012 Phase 4

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL ( 82.75 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.1377 mL 20.6885 mL 41.3770 mL
5 mM 0.8275 mL 4.1377 mL 8.2754 mL
10 mM 0.4138 mL 2.0689 mL 4.1377 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2 mg/mL (8.28 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2 mg/mL (8.28 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2 mg/mL (8.28 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

5-Pyrimidinamine, 4-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-
4-Chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-6-methoxy-2-methyl-5-pyrimidinamine
BE 5895
Moxonidine
BDF 5895
2-(6-Chloro-4-methoxy-2-methylpyrimidin-5-ylamino)-2-imidazoline
Cynt
Lomox
Moxon
Normoxocin
Physiotens
LY 326869
Nucynt
Norcynt
Moxogamma
(4-Chloro-6-methoxy-2-methyl-pyrimidin-5-yl)-imidazolidin-2-ylidene-amine