| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Dantrolene sodium targets the ryanodine receptor (RyR1) in skeletal muscle, specifically inhibiting calcium release from the sarcoplasmic reticulum. By blocking RyR1-mediated calcium release, dantrolene reduces excitation-contraction coupling and decreases muscle contraction. It does not affect neuromuscular transmission or the electrical properties of muscle fibers.
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| ln Vitro |
Dantrolene sodium inhibits calcium-induced calcium release from the sarcoplasmic reticulum in skeletal muscle. In vitro, the compound reduces muscle contractile responses to electrical stimulation and pharmacological agents that induce calcium release. The IC50 for inhibition of calcium release is in the low micromolar range depending on the assay system.
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| ln Vivo |
In vivo, dantrolene sodium produces muscle relaxation by reducing calcium release from the sarcoplasmic reticulum. It is effective in treating malignant hyperthermia, a life-threatening condition triggered by volatile anesthetics and succinylcholine. The compound also reduces muscle spasticity in neurological conditions such as spinal cord injury, multiple sclerosis, and cerebral palsy. Oral administration produces dose-dependent muscle relaxation.
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| Enzyme Assay |
For ryanodine receptor binding assays, skeletal muscle microsomes (heavy sarcoplasmic reticulum) are incubated with [³H]-ryanodine and varying concentrations of dantrolene sodium. Specific binding is determined by subtracting non-specific binding in the presence of excess unlabeled ryanodine. IC50 values are calculated from competition curves.
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| Cell Assay |
For cellular assays, primary skeletal muscle cells or myotubes are loaded with calcium-sensitive fluorescent dyes (e.g., Fluo-4, Fura-2). Cells are treated with dantrolene sodium at various concentrations and stimulated with caffeine or halothane to induce calcium release. Intracellular calcium levels are measured by fluorescence microscopy or flow cytometry.
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| Animal Protocol |
In animal models, dantrolene sodium is administered orally or intravenously. For malignant hyperthermia models, susceptible animals (e.g., pigs or mice) are exposed to halothane and succinylcholine, and dantrolene is administered to reverse the hyperthermic crisis. Body temperature, muscle rigidity, and metabolic parameters (e.g., blood gases, lactate) are monitored. For spasticity models, the compound's effects on muscle tone and reflex activity are assessed.
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| ADME/Pharmacokinetics |
Dantrolene sodium is administered orally or intravenously. Oral bioavailability is approximately 30% due to first-pass metabolism. The compound is metabolized in the liver, primarily by CYP450 enzymes, to 5-hydroxydantrolene, which is excreted in urine and bile. The half-life is approximately 8–12 hours. Dantrolene sodium is protein-bound (>95%).
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation Since there is no information regarding long-term use of dantraline during lactation, alternative medications are recommended, especially when breastfeeding newborns or premature infants. After short-term use, the drug is expected to be cleared from breast milk within 1 to 2 days. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. Dantrolene sodium can cause dose-dependent muscle weakness, drowsiness, dizziness, and gastrointestinal disturbances. Hepatotoxicity is a rare but serious adverse effect, requiring monitoring of liver function during chronic use. The compound is contraindicated in patients with hepatic impairment. At therapeutic doses, the benefits generally outweigh the risks in indicated conditions. |
| Additional Infomation |
Crystals (soluble in DMF aqueous solution). (NTP, 1992)
Dantrolene sodium (anhydrous) is the anhydrous sodium salt of dantrolene. It contains the dantrolene (1-) ligand. Dantrolene sodium is the sodium salt form of dantrolene, a hydantoin derivative and a direct-acting skeletal muscle relaxant. Dantrolene inhibits excitation-contraction coupling in skeletal muscle by binding to rennet receptor 1, thereby reducing intracellular calcium ion concentration. Rennet receptors mediate the release of calcium ions from the sarcoplasmic reticulum, a key step in muscle contraction. Dantrolene is a skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in muscle fibers. It is used to treat spasticity and other neuromuscular abnormalities. Although the mechanism of action of dantrolene may not be central, it is generally classified as a central muscle relaxant. See also: Dantrolene (with active fraction). Dantrolene sodium is a muscle relaxant that inhibits calcium release from the sarcoplasmic reticulum by targeting the ryanodine receptor (RyR1). It is used clinically for malignant hyperthermia, neuroleptic malignant syndrome, and muscle spasticity. The compound is administered orally or intravenously and has a half-life of 8–12 hours. |
| Molecular Formula |
C14H9N4NAO5
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|---|---|
| Molecular Weight |
336.2348
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| Exact Mass |
336.047
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| CAS # |
14663-23-1
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| Related CAS # |
Dantrolene;7261-97-4;Dantrolene sodium hemiheptahydrate;24868-20-0
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| PubChem CID |
6604100
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| Appearance |
Yellow to orange solid powder
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| Boiling Point |
85°C 4mm
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| Melting Point |
534 to 536 °F (NTP, 1992)
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| Flash Point |
283.1ºC
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| LogP |
1.714
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
536
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C(=NC(=O)N1/N=C/C2=CC=C(O2)C3=CC=C(C=C3)[N+](=O)[O-])[O-].[Na+]
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| InChi Key |
KSRLIXGNPXAZHD-HAZZGOGXSA-M
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| InChi Code |
InChI=1S/C14H10N4O5.Na/c19-13-8-17(14(20)16-13)15-7-11-5-6-12(23-11)9-1-3-10(4-2-9)18(21)22;/h1-7H,8H2,(H,16,19,20);/q;+1/p-1/b15-7+;
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| Chemical Name |
sodium;3-[(E)-[5-(4-nitrophenyl)furan-2-yl]methylideneamino]-2-oxo-4H-imidazol-5-olate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9742 mL | 14.8708 mL | 29.7415 mL | |
| 5 mM | 0.5948 mL | 2.9742 mL | 5.9483 mL | |
| 10 mM | 0.2974 mL | 1.4871 mL | 2.9742 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02829268
Conditions:Wolfram Syndrome|Diabetes Mellitus|Optic Nerve Atrophy|AtaxiaLink: https://clinicaltrials.gov/ct2/show/NCT03600376
Conditions:Exertional Heat StrokeProducts are for research use only; We do not sell to patients
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