2229964-07-0
2229964-07-0 structure
- Name: RGLS4326
- Chemical Name: RGLS4326
- CAS Number: 2229964-07-0
- Molecular Formula: C95H115F3N32O51P8S8
- Molecular Weight: 3082.42
- Catalog: Research Areas Cancer
- Create Date: 2022-02-26 19:38:43
- Modify Date: 2025-08-25 17:52:38
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RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM[1].
| Name | RGLS4326 |
|---|
| Description | RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor of microRNA-17 (miR-17). RGLS4326 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD). RGLS4326 inhibits miR-17 function in HeLa cells with an EC50 value of 28.3 nM[1]. |
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| Related Catalog | |
| Target |
MicroRNA[1] |
| In Vitro | RGLS4326, a single-stranded, chemically modified, short oligonucleotide of 9-nt with full complementarity to the miR-17 seed sequence. RGLS4326 inhibits the pathologic functions of the miR-17 family of miRNAs in ADPKD[1]. RGLS4326 treatment inhibits miR-17 function in kidney collecting duct cells in culture as measured by miR-17 PD-Sig, with an EC50 value of 77.2 ± 20.2 nM[1]. RGLS4326 suppresses the growth of primary human autosomal dominant polycystic kidney disease (ADPKD) cysts[1]. Cell Proliferation Assay[1] Cell Line: Primary cysts in 3D Matrigel Concentration: 5, 20, 100, and 300 nM Incubation Time: 9 days Result: Decreased in cyst epithelial cell proliferation. |
| In Vivo | RGLS4326 preferentially distributes to kidney tubules and cysts. RGLS4326 (a single 30 mg/kg SC injection) is rapidly absorbed into plasma, showing Tmax of ≤1 h, Cmax of 8.5 µg/mL, and half-life of <4 h in wild-type mice[1]. In vivo administration of RGLS4326 also upregulates the expression of the direct miR-17 target genes Pkd1 and Pkd2[1]. Animal Model: Pkd2-KO mice[1] Dosage: 20 mg/kg Administration: SC injection Result: Compared to non-cystic control kidneys, polycystic kidneys of PBS-treated Pkd2-KO mice exhibit an age-dependent progressive decline in miR-17 PD-Sig, indicative of increasing miR-17 activity with disease progression. Administration of RGLS4326 reversed this decline in miR-17 PD-Sig, indicating a sustained functional inhibition of miR-17. |
| References |
| Molecular Formula | C95H115F3N32O51P8S8 |
|---|---|
| Molecular Weight | 3082.42 |