MedChemExpress LLC (MCE)

MedChemExpress - Model Dantrolene - 7261-97-4

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].

Dantrolene

MCE China：Dantrolene

Brand：MedChemExpress (MCE)

Cat. No.HY-12542

CAS：7261-97-4

Synonyms：F 368

Purity：98.0%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

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.

In Vitro：Dantrolene (50 μM) sodium alleviates malignant hyperthermia by preventing overactive Ca2+ release by increasing the affinity of ryanodine receptor (RyR) for Mg2+ in rat skin fibers[2]. Dantrolene (30 μM, 1 h-3 days) sodium ameliorates the impairment of neurogenesis and synaptogenesis, in association with restoring intracellular Ca2+ homeostasis and physiological autophagy, cell survival and proliferation in induced pluripotent stem cells derived from patients with Alzheimer's disease [3]. Dantrolene (40 μM, 12 h) sodium enhances the protective effect of hypothermia on cerebral cortex neurons, including improved morphology, increased survival and mitochondrial membrane potential, decreased intracellular reactive oxygen species, cytoplasmic histone-associated DNA fragmentation and apoptosis[7].

In Vivo：Dantrolene (5-20 mg/kg, i.v.) sodium exhibits cardioprotective effects in a rat model of Digoxin (HY-B1049)-induced cardiotoxicity[4]. Dantrolene (5-10 mg/kg, i.p.) sodium attenuates spinal cord inflammation in mice with experimental autoimmune encephalomyelitis (EAE) [5]. Dantrolene (5 mg/kg, intranasal or subcutaneous, 3 times per week) sodium improves cognitive dysfunction in 5XFAD Alzheimer's disease (AD) mice [6].

References：

[1]. 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. [Content Brief]

[2]. 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. [Content Brief]

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

[5]. 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. [Content Brief]

[6]. Shi Y, et al. Intranasal Dantrolene as a Disease-Modifying Drug in Alzheimer 5XFAD Mice. J Alzheimers Dis. 2020;76(4):1375-1389. [Content Brief]

[7]. Xu SY, et al. Dantrolene enhances the protective effect of hypothermia on cerebral cortex neurons. Neural Regen Res. 2015 Aug;10(8):1279-85. [Content Brief]

[8]. 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. [Content Brief]

[9]. 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. [Content Brief]

[10]. Xi Chen, et al. Dantrolene is neuroprotective in Huntington's disease transgenic mouse model. Mol Neurodegener. 2011 Nov 25;6:81. [Content Brief]

[11]. Büyükokuroğlu ME. Anti-inflammatory and antinociceptive properties of Dantrolene in rats and mice. Pharmacol Res. 2002 Jun;45(6):455-60. [Content Brief]

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