| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
| Targets |
Ryanodine receptor type 1 (RyR1). Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor. It acts as a muscle relaxant by reducing calcium release from the sarcoplasmic reticulum.
|
|---|---|
| ln Vitro |
Prior to the addition of caffeine and ryanodine, pretreatment with 20 µM azumolene for one to two minutes suppresses SOCE, which in turn promotes RyR-dependent sarcoplasmic reticulum Ca2+ store depletion in mouse myotubes and adult myofibers [2].
In vitro, Azumolene inhibits calcium release from skeletal muscle sarcoplasmic reticulum. Detailed IC50 values for RyR1 inhibition are available from specialized databases. It has been shown to reduce muscle contracture in preclinical models. |
| ln Vivo |
The effect of Azumolene (EU4093) on twitching in intact rat soleus muscle preparations was practically maximal at a dose of 20 mg/kg. This dose of Azumolene lowered twitch amplitude to 31.9% of control values. Intrafusal muscle contraction, evaluated by spindle afferent discharge responses, is also decreased by Azumolene [1].
In vivo activity data for Azumolene is not extensively detailed in standard references. As a muscle relaxant, it has been investigated for the treatment of malignant hyperthermia and muscle contracture disorders. It offers advantages over dantrolene due to its higher solubility and easier formulation. |
| Enzyme Assay |
In vitro assays for RyR1 antagonism are performed using isolated sarcoplasmic reticulum vesicles or single-channel recordings. Calcium release is measured using fluorescent calcium indicators such as Fluo-4. The compound is added, and the reduction in calcium flux is quantified.
|
| Cell Assay |
In vitro cell-based assays are performed using myoblasts or muscle cell lines. Cells are loaded with calcium-sensitive dyes, and calcium release is stimulated by agonists (e.g., caffeine or halothane). The compound's ability to inhibit calcium release is measured by fluorescence microscopy or plate readers.
|
| Animal Protocol |
In vivo efficacy studies are conducted in animal models of malignant hyperthermia (e.g., susceptible pigs or rodents). Azumolene is administered intravenously or orally. Muscle rigidity, body temperature, and survival are monitored. In muscle contracture models, muscle tension is measured.
|
| ADME/Pharmacokinetics |
Azumolene has a molecular weight of 349.14 and a molecular formula of C13H9BrN4O3. It has higher solubility than dantrolene, which may improve its formulation and bioavailability. It is typically stored in a dry, dark place for one year.
|
| Toxicity/Toxicokinetics |
Detailed toxicological profiles of Azumolene are not extensively reported. As a muscle relaxant, it is expected to have a manageable safety profile. Its higher solubility may reduce the risk of precipitation and local toxicity compared to dantrolene.
|
| References |
|
| Additional Infomation |
Azumoline is a 1,3-oxazole with a 2-position substituted [(2,4-dioxoimidazolidine-1-yl)imino]methyl and a 5-position substituted 4-bromophenyl. It is a muscle relaxant used to treat/prevent malignant hyperthermia. It modulates rennet receptors and has muscle-relaxing effects. It belongs to the 1,3-oxazole, bromobenzene, and imidazolidine-2,4-dione classes. It is the conjugate acid of azumoline (1-).
Azumolene is a research-grade muscle relaxant. It is used to study calcium signaling and muscle contraction. It is not approved for clinical use in most countries. Its molecular formula is C13H9BrN4O3 and its molecular weight is 349.14. |
| Molecular Formula |
C13H9BRN4O3
|
|---|---|
| Molecular Weight |
349.144
|
| Exact Mass |
347.986
|
| Elemental Analysis |
C, 44.72; H, 2.60; Br, 22.89; N, 16.05; O, 13.75
|
| CAS # |
64748-79-4
|
| Related CAS # |
64748-79-4 (free);105336-14-9 (sodium);
|
| PubChem CID |
9568620
|
| Appearance |
White to light brown solid powder
|
| Density |
1.79g/cm3
|
| Index of Refraction |
1.739
|
| LogP |
2.256
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
451
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
BrC1=CC=C(C2=CN=C(/C=N/N3CC(=O)NC3=O)O2)C=C1
|
| InChi Key |
SEGCNGONCZQFDW-OMCISZLKSA-N
|
| InChi Code |
InChI=1S/C13H9BrN4O3/c14-9-3-1-8(2-4-9)10-5-15-12(21-10)6-16-18-7-11(19)17-13(18)20/h1-6H,7H2,(H,17,19,20)/b16-6+
|
| Chemical Name |
2,4-Imidazolidinedione, 1-(((5-(4-bromophenyl)-2-oxazolyl)methylene)amino)-
|
| Synonyms |
EU4093 EU-4093 EU 4093Azumolene
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~13.89 mg/mL (~39.78 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.39 mg/mL (3.98 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.39 mg/mL (3.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.9 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8642 mL | 14.3209 mL | 28.6418 mL | |
| 5 mM | 0.5728 mL | 2.8642 mL | 5.7284 mL | |
| 10 mM | 0.2864 mL | 1.4321 mL | 2.8642 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
