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 also a calcium channel protein inhibitor. Dantrolene inhibits the release of Ca2+ from RyR1 and RyR3, which can be beneficial in a variety of pathologies caused by disruptions in calcium homeostasis (e.g., stroke, ischemia/reperfusion injury, and neurodegenerative diseases) . Dantrolene offers relief of muscle spasms, malignant hyperthermia, and antitoxic, antipyretic, and anti-inflammatory properties[1][2][3][4][5][6][7][8][9][10][11].

Product Specifications

CAS Number

[7261-97-4]

Product Name Alternative

F 368

UNSPSC

12352005

Hazard Statement

H336

Target

Apoptosis; Calcium Channel; Reactive Oxygen Species (ROS)

Type

Reference compound

Related Pathways

Apoptosis; Immunology/Inflammation; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/dantrolene.html

Purity

98.38

Solubility

DMSO : 16.67 mg/mL (ultrasonic; warming; heat to 60°C) |H2O : < 0.1 mg/mL (ultrasonic)

Smiles

O=C1NC(CN1/N=C/C2=CC=C(C3=CC=C([N+]([O-])=O)C=C3)O2)=O

Molecular Formula

C14H10N4O5

Molecular Weight

314.26

Precautions

H336

References & Citations

[1]F Zhao, et al. Dantrolene inhibition of ryanodine receptor Ca2+ release channels. Molecular mechanism and isoform selectivity. J Biol Chem. 2001 Apr 27;276 (17) :13810-6.|[2]Xi Chen, et al. Dantrolene is neuroprotective in Huntington's disease transgenic mouse model. Mol Neurodegener. 2011 Nov 25;6:81.|[3]Christopher B Sylvester, et al. Dantrolene inhibits lysophosphatidylcholine-induced valve interstitial cell calcific nodule formation via blockade of the ryanodine receptor. Front Cardiovasc Med. 2023 Mar 30:10:1112965.|[4]Zhang W, et al. Neuroprotective effects of dantrolene in neurodegenerative disease: Role of inhibition of pathological inflammation. J Anesth Transl Med. 2024 Jun;3 (2) :27-35. |[5]Choi RH, et al. Dantrolene requires Mg2+ to arrest malignant hyperthermia. Proc Natl Acad Sci U S A. 2017 May 2;114 (18) :4811-4815. |[6]Wang Y, et al. Dantrolene Ameliorates Impaired Neurogenesis and Synaptogenesis in Induced Pluripotent Stem Cell Lines Derived from Patients with Alzheimer's Disease. Anesthesiology. 2020 May;132 (5) :1062-1079.|[7]Zardast M, et al. Evaluation of the Effectiveness of Dantrolene against Digoxininduced Cardiotoxicity in Adult Rats. Cardiovasc Hematol Agents Med Chem. 2023;22 (1) :60-65. |[8]Osipchuk NC, et al. Modulation of Ryanodine Receptors Activity Alters the Course of Experimental Autoimmune Encephalomyelitis in Mice. Front Physiol. 2021 Dec 17;12:770820.|[9]Shi Y, et al. Intranasal Dantrolene as a Disease-Modifying Drug in Alzheimer 5XFAD Mice. J Alzheimers Dis. 2020;76 (4) :1375-1389.|[10]Xu SY, et al. Dantrolene enhances the protective effect of hypothermia on cerebral cortex neurons. Neural Regen Res. 2015 Aug;10 (8) :1279-85.|[11]Büyükokuroğlu ME. Anti-inflammatory and antinociceptive properties of Dantrolene in rats and mice. Pharmacol Res. 2002 Jun;45 (6) :455-60.