1. Epigenetics
  2. MicroRNA
  3. RGLS4326

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.

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

5’-AsGsCmAfCfUfUmUsGs-3‘

RGLS4326 Chemical Structure

CAS No. : 2229964-07-0

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1 mg USD 510 In-stock
5 mg USD 1260 In-stock
10 mg USD 2030 In-stock
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & 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].

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

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].

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

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.
Clinical Trial
Molecular Weight

3082.42

Formula

C95H115F3N32O51P8S8

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

5’-AsGsCmAfCfUfUmUsGs-3‘

SMILES

OC[C@@]1(O[C@@H](N2C3=NC=NC(N)=C3N=C2)[C@]4([H])O[C@H]1C)[C@H]4OP(OC[C@]56[C@H]([C@](O[C@H]6C)([H])[C@H](N7C8=C(C(N=C(N8)N)=O)N=C7)O5)OP(OC[C@@H]9[C@H]([C@H]([C@H](N%10C(N=C(C=C%10)N)=O)O9)OC)OP(OC[C@@H]%11[C@H]([C@H]([C@H](N%12C%13=NC=NC(N)=C%13N=C%12)O%11)F)OP(OC[C@@H]%14[C@H]([C@H]([C@H](N%15C(N=C(C=C%15)N)=O)O%14)F)OP(OC[C@@H]%16[C@H]([C@H]([C@H](N%17C(NC(C=C%17)=O)=O)O%16)F)OP(OC[C@@H]%18[C@H]([C@H]([C@H](N%19C(NC(C=C%19)=O)=O)O%18)OC)OP(OC[C@]%20%21[C@H]([C@](O[C@H]%21C)([H])[C@H](N%22C(NC(C=C%22)=O)=O)O%20)OP(OC[C@@]%23%24O[C@@H](N%25C%26=C(C(N=C(N%26)N)=O)N=C%25)[C@@](O[C@H]%24C)([H])[C@@H]%23O)(S)=O)(S)=O)(S)=O)(S)=O)(S)=O)(S)=O)(S)=O)(S)=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 (32.44 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3244 mL 1.6221 mL 3.2442 mL
5 mM 0.0649 mL 0.3244 mL 0.6488 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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
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 0.3244 mL 1.6221 mL 3.2442 mL 8.1105 mL
5 mM 0.0649 mL 0.3244 mL 0.6488 mL 1.6221 mL
10 mM 0.0324 mL 0.1622 mL 0.3244 mL 0.8111 mL
15 mM 0.0216 mL 0.1081 mL 0.2163 mL 0.5407 mL
20 mM 0.0162 mL 0.0811 mL 0.1622 mL 0.4055 mL
25 mM 0.0130 mL 0.0649 mL 0.1298 mL 0.3244 mL
30 mM 0.0108 mL 0.0541 mL 0.1081 mL 0.2704 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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RGLS4326 Related Classifications

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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RGLS4326
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