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  3. Dantrolene sodium hemiheptahydrate

Dantrolene sodium hemiheptahydrate  (Synonyms: Dantrolene sodium hydrate)

Cat. No.: HY-12542A Purity: 99.79%
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Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is also a calcium channel protein inhibitor. Dantrolene sodium hemiheptahydrate 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 sodium hemiheptahydrate 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 sodium hemiheptahydrate Chemical Structure

Dantrolene sodium hemiheptahydrate Chemical Structure

CAS No. : 24868-20-0

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10 mM * 1 mL in DMSO
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Dantrolene sodium hemiheptahydrate:

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Description

Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is also a calcium channel protein inhibitor. Dantrolene sodium hemiheptahydrate 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 sodium hemiheptahydrate 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].

In Vitro

Dantrolene (50 μM) sodium hemiheptahydrate 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 hemiheptahydrate 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 hemiheptahydrate 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.

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 hemiheptahydrate exhibits cardioprotective effects in a rat model of Digoxin (HY-B1049)-induced cardiotoxicity[4].
Dantrolene (5-10 mg/kg, i.p.) sodium hemiheptahydrate attenuates spinal cord inflammation in mice with experimental autoimmune encephalomyelitis (EAE) [5].
Dantrolene (5 mg/kg, intranasal or subcutaneous, 3 times per week) sodium hemiheptahydrate 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

399.31

Formula

C14H16N4NaO8.5

CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

O=C1N([Na])C(CN1/N=C/C2=CC=C(C3=CC=C([N+]([O-])=O)C=C3)O2)=O.[3.5H2O]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (82.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5043 mL 12.5216 mL 25.0432 mL
5 mM 0.5009 mL 2.5043 mL 5.0086 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.5 mg/mL (1.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.5 mg/mL (1.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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 (sealed storage, away from moisture). 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 2.5043 mL 12.5216 mL 25.0432 mL 62.6080 mL
5 mM 0.5009 mL 2.5043 mL 5.0086 mL 12.5216 mL
10 mM 0.2504 mL 1.2522 mL 2.5043 mL 6.2608 mL
15 mM 0.1670 mL 0.8348 mL 1.6695 mL 4.1739 mL
20 mM 0.1252 mL 0.6261 mL 1.2522 mL 3.1304 mL
25 mM 0.1002 mL 0.5009 mL 1.0017 mL 2.5043 mL
30 mM 0.0835 mL 0.4174 mL 0.8348 mL 2.0869 mL
40 mM 0.0626 mL 0.3130 mL 0.6261 mL 1.5652 mL
50 mM 0.0501 mL 0.2504 mL 0.5009 mL 1.2522 mL
60 mM 0.0417 mL 0.2087 mL 0.4174 mL 1.0435 mL
80 mM 0.0313 mL 0.1565 mL 0.3130 mL 0.7826 mL
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  • 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.

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Dantrolene sodium hemiheptahydrate
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