Dantrolene, sodium salt

Ca2+ release inhibitor CAS# 14663-23-1

Dantrolene, sodium salt

Catalog No. BCC6673----Order now to get a substantial discount!

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Dantrolene, sodium salt: 5mg $6 In Stock
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Chemical structure

Dantrolene, sodium salt

3D structure

Chemical Properties of Dantrolene, sodium salt

Cas No. 14663-23-1 SDF Download SDF
PubChem ID 6604100 Appearance Powder
Formula C14H9N4NaO5 M.Wt 336.23
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 10 mM in DMSO
Chemical Name sodium;3-[(E)-[5-(4-nitrophenyl)furan-2-yl]methylideneamino]-2-oxo-4H-imidazol-5-olate
SMILES C1C(=NC(=O)N1N=CC2=CC=C(O2)C3=CC=C(C=C3)[N+](=O)[O-])[O-].[Na+]
Standard InChIKey KSRLIXGNPXAZHD-HAZZGOGXSA-M
Standard InChI 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+;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Dantrolene, sodium salt

DescriptionInhibits release of Ca2+ from sarcoplasmic reticulum via inhibition of ryanodine receptor (RYR) channels. Displays selectivity for RYR1 and RYR3 over RYR2. Protective against the effects of a variety of conditions and agents, including excitatory amino acids. Skeletal muscle relaxant and neuroprotectant.

Dantrolene, sodium salt Dilution Calculator

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Dantrolene, sodium salt Molarity Calculator

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Preparing Stock Solutions of Dantrolene, sodium salt

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9742 mL 14.8708 mL 29.7415 mL 59.4831 mL 74.3539 mL
5 mM 0.5948 mL 2.9742 mL 5.9483 mL 11.8966 mL 14.8708 mL
10 mM 0.2974 mL 1.4871 mL 2.9742 mL 5.9483 mL 7.4354 mL
50 mM 0.0595 mL 0.2974 mL 0.5948 mL 1.1897 mL 1.4871 mL
100 mM 0.0297 mL 0.1487 mL 0.2974 mL 0.5948 mL 0.7435 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Dantrolene, sodium salt

Dantrolene inhibition of ryanodine receptor Ca2+ release channels. Molecular mechanism and isoform selectivity.[Pubmed:11278295]

J Biol Chem. 2001 Apr 27;276(17):13810-6.

As an inhibitor of Ca(2+) release through ryanodine receptor (RYR) channels, the skeletal muscle relaxant dantrolene has proven to be both a valuable experimental probe of intracellular Ca(2+) signaling and a lifesaving treatment for the pharmacogenetic disorder malignant hyperthermia. However, the molecular basis and specificity of the actions of dantrolene on RYR channels have remained in question. Here we utilize [(3)H]ryanodine binding to further investigate the actions of dantrolene on the three mammalian RYR isoforms. The inhibition of the pig skeletal muscle RYR1 by dantrolene (10 microm) was associated with a 3-fold increase in the K(d) of [(3)H]ryanodine binding to sarcoplasmic reticulum (SR) vesicles such that dantrolene effectively reversed the 3-fold decrease in the K(d) for [(3)H]ryanodine binding resulting from the malignant hyperthermia RYR1 Arg(615) --> Cys mutation. Dantrolene inhibition of the RYR1 was dependent on the presence of the adenine nucleotide and calmodulin and reflected a selective decrease in the apparent affinity of RYR1 activation sites for Ca(2+) relative to Mg(2+). In contrast to the RYR1 isoform, the cardiac RYR2 isoform was unaffected by dantrolene, both in native cardiac SR vesicles and when heterologously expressed in HEK-293 cells. By comparison, the RYR3 isoform expressed in HEK-293 cells was significantly inhibited by dantrolene, and the extent of RYR3 inhibition was similar to that displayed by the RYR1 in native SR vesicles. Our results thus indicate that both the RYR1 and the RYR3, but not the RYR2, may be targets for dantrolene inhibition in vivo.

Dantrolene inhibits long-term depression and depotentiation of synaptic transmission in the rat dentate gyrus.[Pubmed:8577362]

Neuroscience. 1995 Oct;68(3):621-4.

The involvement of Ca release from intracellular stores in the induction of long-term depression and depotentiation of excitatory synaptic transmission was investigated in the rat dentate gyrus using dantrolene, an agent known to block Ca release via the ryanodine receptor. In control slices, low-frequency stimulation (1 Hz for 15 min) induced robust long-term depression of baseline field excitatory postsynaptic potentials and depotentiation of previously established long-term potentiation. Dantrolene (50 microM) was found to block completely both long-term depression of baseline responses and depotentiation. Moreover, long-term potentiation induced by high-frequency stimulation was enhanced in the presence of dantrolene.

Dantrolene ameliorates the metabolic hallmarks of sepsis in rats and improves survival in a mouse model of endotoxemia.[Pubmed:8159702]

Proc Natl Acad Sci U S A. 1994 Apr 12;91(8):3039-43.

Sepsis is the systemic inflammatory response resulting from serious infection and is the most common cause of death in intensive care units. Intracellular free calcium concentration ([Ca2+]i) is an important regulator of numerous cellular processes and when increased excessively may act as a potent cellular toxin. To determine if [Ca2+]i is responsible for the major metabolic changes which are hallmarks of sepsis, we examined if sodium dantrolene, a drug which decreases release of calcium from sarcoplasmic reticulum, affected the metabolic abnormalities in plasma and epitrochlearis muscles of rats made septic by cecal ligation and perforation. Dantrolene when added in vitro or when given in vivo decreases many of the metabolic hallmarks of sepsis--i.e., muscle protein breakdown approximately 30%, muscle glucose transport approximately 38%, muscle lactate formation approximately 28%, and plasma lactate approximately 29% (P < 0.05). In addition, we examined the ability of dantrolene to improve survival in a mouse model of endotoxemia. Dantrolene caused > 2-fold improvement in survival when it was administered concurrently with endotoxin (54% vs. 20% survival in dantrolene-treated and control mice, respectively (P < 0.001). Our results are consistent with the hypothesis that an increase in [Ca2+]i plays an important role in the metabolic abnormalities which occur during sepsis and that dantrolene administration may be an effective therapeutic strategy.

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