2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. Calcium Channel Reactive Oxygen Species (ROS) Apoptosis
  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 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.

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CAS No. : 7261-97-4

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Based on 15 publication(s) in Google Scholar

Other Forms of Dantrolene:

Dantrolene Related Antibodies

Top Publications Citing Use of Products

    Dantrolene purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Nov 18;16(1):10110.  [Abstract]

    Dose-dependent effects of Dantrolene (DAN) and AZU on ER luminal [Ca2+] changes in cell lines expressing RyR1 R2163C. The reslts showed that effectively Dantrolene (DAN) inhibited Ca2+ leakage, with IC50 value of 0.26 μM.

    Dantrolene purchased from MedChemExpress. Usage Cited in: J Cell Commun Signal. 2023 Dec;17(4):1309-1321.  [Abstract]

    Effect of 2 µM LETX-VI treatment on cytosolic Ca2+ level when RyRs in ER membrane was inhibited by Dantrolene (30 µM). The results demonstrated that blockade of RyR by Dantrolene decreased the F340/F380 ratio, indicating that RyR is involved in LETX-VI-induced Ca2+ release from the endoplasmic reticulum.

    View All Calcium Channel Isoform Specific Products:

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    N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

    • Biological Activity

    • Purity & Documentation

    • References

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    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].

    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 and measured every 10 secs for 300 secs by time lapse fluorimetry based Michelis-Menten analysis
    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 and measured every 10 secs for 300 secs by time lapse fluorimetry based Michelis-Menten analysis
    		[PMID: 31299492]
    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].

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

    Dantrolene Related Antibodies

    Cell Differentiation Assay[3]

    Cell Line: Induced pluripotent stem cells from patients with familiar and sporadic Alzheimer’s disease
    Concentration: 30 μM
    Incubation Time: 3 days
    Result: Promoted differentiation of neuroprogenitor cell derived from sporadic Alzheimer’s disease/familial Alzheimer’s disease induced pluripotent stem cells into immature neurons at differentiation day 23.
    Promoted the percentage of Trb1 positive cells.
    Promoted differentiation into basal forebrain cholinergic neurons.
    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].

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

    Animal Model: C57BL/6 male mice (EAE was induced by subcutaneous administration of a total of 300 μg in the flanks (each flank received 150 μg) of rodent myelin oligodendrocyte glycoprotein peptide 35–55 (MEVGWYRSPFSRVVHLYRNGK, New England Peptide) emulsified in the complete Freund’s adjuvant containing Mycobacterium tuberculosis H37Ra[5]
    Dosage: 5, 10 mg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Reduced the severity of EAE clinical symptoms and dampened inflammation in the spinal cord
    Caused skeletal muscle weakness at 5 mg/kg.
    Did not display noticeable upright movement deficits on flat-surface at 5 mg/kg.
    Molecular Weight

    314.26

    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 3.1821 mL 15.9104 mL 31.8208 mL
    5 mM 0.6364 mL 3.1821 mL 6.3642 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.

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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:

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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: 98.38%

    SDS (393 KB)

    COA (248 KB) HNMR (131 KB) RP-HPLC (257 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 3.1821 mL 15.9104 mL 31.8208 mL 79.5520 mL
    5 mM 0.6364 mL 3.1821 mL 6.3642 mL 15.9104 mL
    10 mM 0.3182 mL 1.5910 mL 3.1821 mL 7.9552 mL
    15 mM 0.2121 mL 1.0607 mL 2.1214 mL 5.3035 mL
    20 mM 0.1591 mL 0.7955 mL 1.5910 mL 3.9776 mL
    25 mM 0.1273 mL 0.6364 mL 1.2728 mL 3.1821 mL
    30 mM 0.1061 mL 0.5303 mL 1.0607 mL 2.6517 mL
    40 mM 0.0796 mL 0.3978 mL 0.7955 mL 1.9888 mL
    50 mM 0.0636 mL 0.3182 mL 0.6364 mL 1.5910 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 ChannelReactive Oxygen Species (ROS)ApoptosisCa2+ channelsCa channelsorallynon-competitiveglutathione reductaseryanodine receptorRyRCa2+muscle spasticitymalignant hyperthermiaHuntington's diseaseneuroleptic malignant syndromeInhibitorinhibitorinhibit

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