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

Cat. No.: HY-114231C: FAQs
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Exaluren (ELX-02) sulfate is an investigational, advanced synthetic eukaryotic ribosome selective glycoside (ERSG). Exaluren sulfate is being developed as a therapy for genetic diseases caused by nonsense mutations.

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

Exaluren sulfate Chemical Structure

CAS No. : 1375073-94-1

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Other Forms of Exaluren sulfate:

Exaluren Get quote
Exaluren disulfate Get quote

1 Publications Citing Use of MCE Exaluren sulfate

•Mol Ther. 2023 Jan 13;S1525-0016(23)00014-X. [Abstract]

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	1493 μM Compound: (S)-9	Inhibition of mitochondrial ribosome-mediated protein synthesis in human HeLa cells assessed as {35S]methionine incorporation by autoradiography Inhibition of mitochondrial ribosome-mediated protein synthesis in human HeLa cells assessed as {35S]methionine incorporation by autoradiography	[PMID: 23148581]

In Vitro

Exaluren (ELX-02) sulfate (100-400 μg/mL) is not toxic, and permits read-through of nonsense mutations in human cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	Wildtype human proximal tubule cells (HK-2)
Concentration:	0, 100 and 400 μg/mL
Incubation Time:	0, 24, 48 and 72 h
Result:	Cytotoxicity assay in wildtype human proximal tubule cells (HK-2) showing no toxic effect of 400 μg/mL at 0, 24, 48 and 72 h.

In Vivo

Exaluren (ELX-02) sulfate (10 and 30 mg/kg; repeat subcutaneous administration; twice weekly, total of 8 doses) shows accumulation in tissues that is dose dependent without gender difference^[1].
In plasma Exaluren (ELX-02) sulfate is rapidly absorbed with a T_max of 0.25 h after both single (a single subcutaneous injection at 10 mg/kg at dose volume of 5 mL/kg) and repeated administration (twice weekly with 10 mg/kg/dose for 21 days; total of 7 administrations). Exaluren (ELX-02) sulfate is rapidly eliminated from plasma in a biphasic manner with the terminal half-life (T_1/2) of 0.5 h^[1].
In a Ctns^Y226X nonsense mutant mouse, subcutaneous Exaluren (ELX-02) sulfate accumulates in kidney tissue without overt renal toxicity and that Exaluren (ELX-02) sulfate (10 mg/kg X2/week for 3 weeks) reduces renal cystine accumulation in vivo^[1].

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

Animal Model:	Twenty-nine CtnsY226X/Y226X mice 5-7 month old^[1]
Dosage:	10 and 30 mg/kg
Administration:	Subcutaneous injection, at dose volume of 5 mL/kg, twice weekly for a period of 28 days (total of 8 doses)
Result:	Highest levels were measured in the kidney, followed by spleen and liver, with lower levels in other tissues (lung, heart, cochlea and brain).

Clinical Trial

Molecular Weight

580.60

Formula

C₁₉H₄₀N₄O₁₄S

CAS No.

1375073-94-1

SMILES

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.[x]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Leubitz A, et al. Safety, Tolerability, and Pharmacokinetics of Single Ascending Doses of ELX-02, a Potential Treatment for Genetic Disorders Caused by Nonsense Mutations, in Healthy Volunteers. Clin Pharmacol Drug Dev. 2019 Jan 16. [Content Brief]

Exaluren sulfate Related Classifications

Metabolic Disease

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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.

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