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Dantrolene (Synonyms: F 368)

Cat. No.: HY-12542
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Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.

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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Description

Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome[1][2][3][4][5].

In Vitro

Dantrolene interferes with calcium release from the sarcoplasmic reticulum and thus to inhibit excitation--contraction coupling[1].
Dantrolene acts directly on the RYR1 to reduce the extent of channel activation by calmodulin (CaM) and thereby decreases the Ca2+ sensitivity of channel activation[2].
Dantrolene inhibits abnormal Ca2+ release from the sarcoplasmic reticulum[3].
Dantrolene depresses excitation-contraction coupling in muscle fibers by inhibiting calcium release from the sarcoplasmic reticulum[3].
Dantrolene also shows calcium channel blocker effect in the smooth muscle membrane as well as antioxidative and cytoprotective properties[3].
Dantrolene affects the membrane calcium channel of smooth muscle cells and inhibits calcium influx[3].
Dantrolene is a skeletal muscle-specific muscle relaxant that works on the cardiac muscle. Dantrolene (0.3 μM) binds to domain 601-620 of RyR2 and corrects defective inter-domain interaction within RyR2 in failing hearts. This in turn inhibits spontaneous Ca2++ leak/Ca2+ sparks, and improves cardiomyocyte function in failing hearts[4].

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

In Vivo

Dantrolene is neuroprotective in Huntington's disease transgenic mouse model[5].
Feeding dantrolene (5 mg/kg) twice a week to YAC128 mice between 2 months and 11.5 months of age resulted in significantly improved performance in the beam-walking and gait-walking assays[5].

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

Animal Model: YAC128 transgenic mice (FVBN/NJ background strain) and WT mice[5]
Dosage: 5 mg/kg
Administration: Fed orally twice per week from 2 to 11.5 months of age, followed by a washout period of 2 months (13.5 months of age)
Result: Resulted in significantly improved performance in the beam-walking and gait-walking assays.
Molecular Weight

314.25

Formula

C14H10N4O5

CAS No.
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 Vivo:
  • 1.

    Dantrolene is suspended in 50 μL of PBS with 2% corn flour[5].

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