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  3. Exaluren disulfate

Exaluren disulfate  (Synonyms: ELX-02 disulfate; NB-124 disulfate)

Cat. No.: HY-114231B Purity: ≥98.0%
Handling Instructions Technical Support

Exaluren (ELX-02; NB-124) disulfate is an synthetic eukaryotic ribosome-selective glycoside that induces read-through of nonsense mutations, resulting in normally localized full-length functional proteins. Exaluren disulfate is used for the research of cystic fibrosis caused by nonsense mutations.

For research use only. We do not sell to patients.

Exaluren disulfate

Exaluren disulfate Chemical Structure

CAS No. : 2244622-33-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in Water In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
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100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Exaluren disulfate:

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  • Biological Activity

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  • References

  • Customer Review

Description

Exaluren (ELX-02; NB-124) disulfate is an synthetic eukaryotic ribosome-selective glycoside that induces read-through of nonsense mutations, resulting in normally localized full-length functional proteins. Exaluren disulfate is used for the research of cystic fibrosis caused by nonsense mutations[1][2].

In Vitro

Exaluren disulfate induces significant premature stop codon read-through with maintained native stop codon fidelity in DMS-114 cells, increasing p53 protein expression and reducing nonsense-mediated mRNA decay of TP53 mRNA[1].
Exaluren disulfate exhibits consistent nonsense mutation read-through activity and efficacy in human bronchial epithelial cells, Fischer rat thyroid cells, and a dual luciferase cystic fibrosis model[1].
Exaluren disulfate induces read-through of the CTNS W138X nonsense allele in human cystinosis fibroblasts, increasing cystinosin protein and CTNS mRNA levels while reducing half-cystine levels[1].

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

In Vivo

Exaluren (30-60 mg/kg; s.c.; daily; 14 days) disulfate achieves superior CFTR functional rescue in a CF mouse model expressing a human CFTRG542X transgene[1].
Exaluren (10 mg/kg; s.c.; 7 injections over a 3-week period) disulfate reduces kidney cell cystine levels by 30% in CTNSY226X nonsense mutant mice without overt renal toxicity[1].

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

Animal Model: CF mouse model expressing a human CFTRG542X transgene[1]
Dosage: 30, 60 mg/kg
Administration: s.c.; daily; 14 days
Result: Achieved CFTR functional rescue superior to gentamicin and exhibited favorable pharmacodynamic properties.
Molecular Weight

678.68

Formula

C19H42N4O18S2

CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

OS(=O)(O)=O.C[C@@H](O)[C@@]([C@@H](O)[C@H](O)[C@H]1N)([H])O[C@]1([H])O[C@H]([C@H](C[C@@H](N)[C@@H]2O)N)[C@]2([H])O[C@@H]3O[C@@]([C@@H](N)C)([H])[C@@H](O)[C@H]3O.OS(=O)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (147.34 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4734 mL 7.3672 mL 14.7345 mL
5 mM 0.2947 mL 1.4734 mL 2.9469 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (147.34 mM); Clear solution; Need ultrasonic

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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

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 (stored under nitrogen). 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
H2O 1 mM 1.4734 mL 7.3672 mL 14.7345 mL 36.8362 mL
5 mM 0.2947 mL 1.4734 mL 2.9469 mL 7.3672 mL
10 mM 0.1473 mL 0.7367 mL 1.4734 mL 3.6836 mL
15 mM 0.0982 mL 0.4911 mL 0.9823 mL 2.4557 mL
20 mM 0.0737 mL 0.3684 mL 0.7367 mL 1.8418 mL
25 mM 0.0589 mL 0.2947 mL 0.5894 mL 1.4734 mL
30 mM 0.0491 mL 0.2456 mL 0.4911 mL 1.2279 mL
40 mM 0.0368 mL 0.1842 mL 0.3684 mL 0.9209 mL
50 mM 0.0295 mL 0.1473 mL 0.2947 mL 0.7367 mL
60 mM 0.0246 mL 0.1228 mL 0.2456 mL 0.6139 mL
80 mM 0.0184 mL 0.0921 mL 0.1842 mL 0.4605 mL
100 mM 0.0147 mL 0.0737 mL 0.1473 mL 0.3684 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Exaluren disulfate
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HY-114231B
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