Dantrolene

• Product Name Alternative:

  F 368

• UNSPSC 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 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].

• Target Antigen:

  Apoptosis; Calcium Channel; Reactive Oxygen Species

• Type:

  Reference compound

• Related Pathways:

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

• Field of Research:

  Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

• Assay Protocol:

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

• Purity:

  98.0

• 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 Weight:

  314.257

• 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. J Cell Commun Signal. 2023 Sep 13.|Res Sq. 2024 Jun 11.|ACS Omega. 2020 Oct 12;5(41):26551-26561.|J Anim Sci Biotechnol. 2022 Feb 11;13(1):9.|Research Square Preprint. 2021 May.|Anim Nutr. 28 September 2021.|Cell Res. 2022 Mar;32(3):288-301.|Front Immunol. 2021 Jul 7;12:688674.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Launched

• CAS Number:

  7261-97-4