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

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
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Dantrolene:

Dantrolene Related Antibodies

Top Publications Citing Use of 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

  • 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 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
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 (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.
Clinical Trial
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.

  • Molarity Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

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 (247 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 SpeciesApoptosisCa2+ channelsCa channelsorallynon-competitiveglutathione reductaseryanodine receptorRyRCa2+muscle spasticitymalignant hyperthermiaHuntington's diseaseneuroleptic malignant syndromeInhibitorinhibitorinhibit

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