| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
Dantrolene (60 μM; Days 1 and 3) In paVIC, sodium heptahydrate dramatically reduces the expression of ACTA2 while increasing the expression of RUNX2 [2]. The creation of paVIC calcified nodules triggered by 10 μM lysophosphatidylcholine (LPC) is inhibited by dantrolene (10, 30, 60 μM) sodium hemiheptahydrate [2].
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|---|---|
| ln Vivo |
Dantrolene three times a week at a dosage of 5 mg/kg In tests of gait and balance beam walking, sodium hexahydrate enhances performance [3]. (10 mg/kg; intraperitoneal; three days a week; for 40–60 days) Significant improvements in gait, decreased LC3-II levels, enhanced mitochondrial ATP synthesis, and decreased brain activation were observed with sodium heptahydrate. In the brain of neuropathic Gaucher illness, dantrolene sodium hemiheptahydrate decreases autophagy and the expression of CALM (calmodulin). [4]
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| Cell Assay |
RT-PCR[2]
Cell Types: porcine aortic valve interstitial cells (paVIC) Tested Concentrations: 60 μM Incubation Duration: 1 day and 3 days Experimental Results: Dramatically inhibited ACTA2 expression and upregulated RUNX2 expression. |
| Animal Protocol |
Animal/Disease Models: YAC128 transgenic mice (FVBN/NJ background strain) and WT mice [3 ]
Doses: 5 mg/kg Route of Administration: Oral twice weekly from 2 months of age to 11.5 months of age Experimental Results: Result in significant improvement in performance. Beam walking and gait walking assays. Dramatically diminished the loss of NeuN-positive striatal neurons and diminished the formation of Httexp nuclear aggregates. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Because no information is available on the long-term use of dantrolene during breastfeeding, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. After short-term use, the drug would be expected to be eliminated from milk in 1 to 2 days. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| References |
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| Additional Infomation |
Crystals (in aqueous DMF). (NTP, 1992)
Dantrolene sodium (anhydrous) is the anhydrous sodium salt of dantrolene. It contains a dantrolene(1-). Dantrolene Sodium is the sodium salt form of dantrolene, a hydantoin derivative and direct-acting skeletal muscle relaxant. Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1, and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. Skeletal muscle relaxant that acts by interfering with excitation-contraction coupling in the muscle fiber. It is used in spasticity and other neuromuscular abnormalities. Although the mechanism of action is probably not central, dantrolene is usually grouped with the central muscle relaxants. See also: Dantrolene (has active moiety). |
| Molecular Formula |
C14H10N4NAO5
|
|---|---|
| Molecular Weight |
337.2428
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| Exact Mass |
336.047
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| CAS # |
24868-20-0
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| Related CAS # |
Dantrolene;7261-97-4;Dantrolene sodium;14663-23-1
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| PubChem CID |
6604100
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| Appearance |
Yellow to orange solid powder
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| Boiling Point |
544.5ºC at 760mmHg
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| Melting Point |
>230ºC
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| Flash Point |
283.1ºC
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| Vapour Pressure |
1.09E-12mmHg at 25°C
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| LogP |
2.978
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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) |
DMSO : ≥ 33 mg/mL (~82.64 mM)
H2O : < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (1.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 5.0 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: ≥ 0.5 mg/mL (1.25 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 5.0 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 | 2.9652 mL | 14.8262 mL | 29.6525 mL | |
| 5 mM | 0.5930 mL | 2.9652 mL | 5.9305 mL | |
| 10 mM | 0.2965 mL | 1.4826 mL | 2.9652 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.
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