2. Membrane Transporter/Ion Channel Neuronal Signaling Autophagy
  3. Calcium Channel Autophagy
  4. Dantrolene

Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.

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

Dantrolene Chemical Structure

Dantrolene Chemical Structure

CAS No. : 7261-97-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 72 In-stock
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10 mM * 1 mL in DMSO USD 72 In-stock
Solid
5 mg USD 65 In-stock
10 mg USD 92 In-stock
25 mg USD 130 In-stock
50 mg USD 210 In-stock
100 mg USD 270 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Dantrolene:

Dantrolene Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
0.059 μM
Compound: Dantrolene
Inhibition of RyR1 harboring R2163C mutant (unknown origin) stably expressed in HEK293 cells coexpressing R-CEPIA1er assessed as suppression in Ca2+ leakage from ER prestimulated with doxycycline for 24 to 28 hrs followed by compound addition at 100 secs
Inhibition of RyR1 harboring R2163C mutant (unknown origin) stably expressed in HEK293 cells coexpressing R-CEPIA1er assessed as suppression in Ca2+ leakage from ER prestimulated with doxycycline for 24 to 28 hrs followed by compound addition at 100 secs
[PMID: 31299492]
In Vitro

Dantrolene (60 μM; at 1 and 3 days) significantly inhibits ACTA2 expression and upregulats RUNX2 expression in paVICs[2].
Dantrolene (60 μM; overnight pretreatment) inhibits LPC-induced calcium flux in porcine aortic valve interstitial cells[2].
Dantrolene (10, 30, 60 μM) inhibited calcific nodule formation of paVICs due to 10 μM lysophosphatidylcholine (LPC)[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Dantrolene Related Antibodies

RT-PCR[2]

Cell Line: Porcine aortic valvular interstitial cells (paVICs)
Concentration: 60 μM
Incubation Time: At 1 and 3 days
Result: Significantly inhibited ACTA2 expression and upregulated RUNX2 expression.
In Vivo

Dantrolene (5 mg/kg; fed orally twice per week) improves performance in the beam-walking and gait-walking assay[3].
Dantrolene (10 mg/kg; IP; three days per week; for 40-60 days) significantly improves gait, reduces LC3-II levels, improves mitochondrial ATP production and reduced inflammation in the brain. Dantrolene partially reduces autophagy and the expression of CALM (calmodulin) in the brain of neuronopathic Gaucher disease mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: YAC128 transgenic mice (FVBN/NJ background strain) and WT mice[3]
Dosage: 5 mg/kg
Administration: Fed orally twice per week from 2 to 11.5 months of age
Result: Resulted in significantly improved performance in the beam-walking and gait-walking assays.
Significantly reduced the loss of NeuN-positive striatal neurons and reduced formation of Httexp nuclear aggregates.
Clinical Trial
Molecular Weight

314.25

Formula

C14H10N4O5
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NC(CN1/N=C/C2=CC=C(C3=CC=C([N+]([O-])=O)C=C3)O2)=O
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 : 16.67 mg/mL (53.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1822 mL 15.9109 mL 31.8218 mL
5 mM 0.6364 mL 3.1822 mL 6.3644 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

  • Protocol 1

    Dantrolene is suspended in 50 μL of PBS with 2% corn flour[5].

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

SDS (393 KB)

COA (248 KB) HNMR (131 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1822 mL 15.9109 mL 31.8218 mL 79.5545 mL
5 mM 0.6364 mL 3.1822 mL 6.3644 mL 15.9109 mL
10 mM 0.3182 mL 1.5911 mL 3.1822 mL 7.9554 mL
15 mM 0.2121 mL 1.0607 mL 2.1215 mL 5.3036 mL
20 mM 0.1591 mL 0.7955 mL 1.5911 mL 3.9777 mL
25 mM 0.1273 mL 0.6364 mL 1.2729 mL 3.1822 mL
30 mM 0.1061 mL 0.5304 mL 1.0607 mL 2.6518 mL
40 mM 0.0796 mL 0.3978 mL 0.7955 mL 1.9889 mL
50 mM 0.0636 mL 0.3182 mL 0.6364 mL 1.5911 mL
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Dantrolene Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dantrolene7261-97-4F 368F368F-368Calcium ChannelAutophagyCa2+ channelsCa channelsorallynon-competitiveglutathione reductaseryanodine receptorRyRCa2+muscle spasticitymalignant hyperthermiaHuntington's diseaseneuroleptic malignant syndromeInhibitorinhibitorinhibit

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