Art. -Nr.: HY-139290

RGLS4326

Name: RGLS4326
Brand: MedChemExpress
SKU: HY-139290
Price: 510.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: RG4326)

1 Cited Publications

Kundenbewertung

Based on 1 publication(s) in Google Scholar

RGLS4326 (RG4326) is a microRNA-17 (miR-17) oligonucleotide inhibitor with an EC₅₀ of 28.3 nM. RGLS4326 antagonizes AMPAR and inhibits ligand binding. RGLS4326 relieves the inhibition of Pkd1/Pkd2 by miR-17 and upregulates PC1/PC2. RGLS4326 preferentially distributes to the kidney and cysts, attenuates cyst progression and improves survival in mouse models of autosomal dominant polycystic kidney disease (ADPKD) in a miR-17 binding motif-dependent manner. RGLS4326 can be used in ADPKD-related research.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.06%
CAS. Nr.: 2229964-07-0
Formel: C₉₅H₁₁₅F₃N₃₂O₅₁P₈S₈
Molecular Weight:3082.42

Speicherung:

-20°C, stored under nitrogen

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

RGLS4326 Chemical Structure

CAS. Nr.: 2229964-07-0

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Publications Citing Use of MedChemExpress (MCE) RGLS4326

Patent. US20250283086A1.

Customer Validation & Images

Bio/Physico-chemical AssayWB

Bio/Physico-chemical Assay
WB

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle iGluR Isoform-spezifische Produkte anzeigen :

In Vitro

Glutamate Release or ReceptorsCytokines & ChemokinesMitochondrial FunctionRenal RegulationOthers

Glutamate Release or Receptors

RGLS4326 competitively antagonizes human GluA1/GluA4 AMPAR in HEK293 cells with K_b = 163 nM^[1].
RGLS4326 inhibits the function of GluA2-homotetrameric AMPARs in HEK293 cells^[1].
RGLS4326 (200 µM; 30 min) binds GluA2-γ2 LBD via 3’G, stabilizes the open clamshell/closed pore state, and provides the structural basis for competitive AMPAR inhibition^[1].

Glutamate Release or Receptors

Cytokines & Chemokines

RGLS4326 (10-100 μM; 90 min) is a cell-free AMPA receptor ligand that inhibits [3H]-AMPA binding with an IC₅₀ <10 μM through its 3'-terminal guanine^[1].

Mitochondrial Function

RGLS4326 (100 μM) derepresses Pkd1/Pkd2 and inhibits 3D cyst growth in Pkd1^RC/- mouse collecting duct-derived cells^[2].
RGLS4326 shows no in vitro genotoxicity or mitochondrial toxicity in bacterial mutagenicity, human lymphocyte micronucleus, and human cell assays^[3].

Renal Regulation

RGLS4326 inhibits miR-17 and de-represses Pkd1/Pkd2 in mouse kidney collecting duct cells with an EC₅₀ of 77.2 nM^[3].
RGLS4326 (5-10 μM; 24-72 h) derepresses miR-17 PD-Sig in isolated mouse kidney slices and shows low pro-inflammatory gene induction in rat tissue slices^[3].
RGLS4326 (8 days) derepresses miR-17 targets, increasing PC1 by approximately 2-fold and PC2 by approximately 4-fold, and reduces cyst growth in primary human ADPKD cyst cultures^[3].

Others

RGLS4326 retains targeted anti-miR-17 activity in in vitro ADPKD models, de-represses PKD1/PKD2, and reduces cyst growth^[1].
RGLS4326 is metabolically stable in mouse, monkey, and human tissue lysates^[3].
RGLS4326 (10 μM; 24 h) inhibits miR-17 and derepresses the miR-17 luciferase sensor in HeLa cells with an EC₅₀ of 28.3 nM^[3].

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

Real Time qPCR^[3]

Cell Line:

Ex vivo mouse kidney slices
Concentration:

10 μM
Incubation Time:

72 h
Result:

De-repressed miR-17 PD-Sig in ex vivo mouse kidney slices.
RNA extraction and qRT-PCR analysis revealed a consistent shift in the characteristic expression profiles of target genes, which was consistent with the restoration of the miR-17 pathway.

Real Time qPCR^[3]

Cell Line:

Rat liver and kidney sections
Concentration:

5 μM
Incubation Time:

24 and 48 h
Result:

Following RNA extraction, qRT-PCR analysis revealed only low-level induction of the pro-inflammatory gene panel in both tissues.
Did not elicit robust upregulation of Il1b, Tnf, or Ccl2 relative to Vehicle-treated slices.

In Vivo

Renal Regulation

RGLS4326 (0.003-300 mg/kg; s.c.; single injection) induces stronger and more durable miR-17 target engagement in the kidney than in the liver^[1].
RGLS4326 (20 mg/kg; s.c.; injected on postnatal days P8, P10, P12, and P15 (4 doses)) shows in vivo activity similar to that of RGLS8429 (HY-150364) in the Pkd1^F/RC ADPKD mouse model, significantly alleviating kidney enlargement, cyst progression, cell proliferation, and renal function impairment^[1].
RGLS4326 (20 mg/kg; s.c.; injected at P10-P16) almost prevents PKD and preserves renal function by P18 in KspCre; Pkd1^F/RC mice^[2].
RGLS4326 (20 mg/kg; s.c.; injected at P16-P17) attenuates PKD progression and stabilizes renal function by P26 in KspCre; Pkd1^F/RC mice^[2].
RGLS4326 (20 mg/kg; subcutaneous injection; at P16-P17, then weekly or biweekly until 18 weeks of age) improves survival and preserves renal parenchyma by 18 weeks in KspCre; Pkd1^F/RC mice^[2].
RGLS4326 (30 mg/kg; s.c.; single dose) persistently displaces renal miR-17 from translationally active polysomes in normal mice^[3].
RGLS4326 (30 mg/kg; s.c.; single dose) inhibits renal miR-17 in the JCK/C57BL6 PKD and Pcy/CD1 PKD models^[3].
RGLS4326 (20 mg/kg; s.c.; injected on postnatal days 10-19) inhibits miR-17 and reduces cystic kidney disease progression in Pkd2-KO mice^[3].
RGLS4326 (25 mg/kg; s.c.; QW or Q4W; 25 weeks) reduces cyst burden in Pcy/CD1 mice when administered early, whereas late intervention is ineffective^[3].
RGLS4326 (1-25 mg/kg; s.c.; QW; 9 weeks) dose-dependently reduces kidney weight-to-body weight ratio and cyst index in Pcy/DBA mice, whereas monthly dosing is ineffective^[3].
RGLS4326 (30 mg/kg; s.c.; QW; 8 weeks) slows the increase in kidney volume measured by MRI in Pcy/DBA mice^[3].

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

Animal Model:

C57BL6^[1]
Dosage:

0.003, 0.03, 0.3, 3, 30, or 300 mg/kg
Administration:

s.c.; single injection
Result:

Showed stronger target engagement in kidney (≥75% for 14 days) than in liver (≤75% by 7 days).
Exhibited similar potency in the kidney.

Animal Model:

Ksp/Cre; Pkd1^F/RC (postnatal day 8-18)^[1]
Dosage:

20 mg/kg
Administration:

s.c.; on postnatal days P8, P10, P12, and P15 (4 doses)
Result:

Showed a similar efficacy profile to RGLS8429 in the Pkd1^F/RC ADPKD mouse model after repeat s.c. dosing at 20 mg/kg.
Resulted in a significant reduction in KW/BW, the cyst index, the proliferation index, and BUN levels, and improved renal pathological morphology.

Animal Model:

KspCre; Pkd1F/RC (C57BL/6J background; equal numbers of males and females)^[2]
Dosage:

20 mg/kg
Administration:

subcutaneous injection; on P10, P11, P12, and P16
Result:

By P18, PKD was virtually prevented, and renal function remained normal in Pkd1RC/- mice.

Animal Model:

KspCre; Pkd1F/RC (C57BL/6J background; equal numbers of males and females)^[2]
Dosage:

20 mg/kg
Administration:

subcutaneous injection; on P16 and P17
Result:

By P26, Pkd1RC/- mice exhibited attenuation of PKD progression and stabilization of kidney function.

Animal Model:

KspCre; Pkd1F/RC (C57BL/6J background; equal numbers of males and females)^[2]
Dosage:

20 mg/kg (weekly); 20 mg/kg (semimonthly)
Administration:

subcutaneous injection; on P16 and P17, then weekly until 18 weeks of age; or subcutaneous injection; on P16 and P17, then every other week (semimonthly) until 18 weeks of age
Result:

70% (7/10) of mice receiving every-other-week dosing and 50% (5/10) of mice receiving weekly dosing survived until 18 weeks of age.
Surviving mice had substantially preserved kidney parenchyma and reduced KW/BW.

Animal Model:

C57BL/6 (WT/C57BL6)^[3]
Dosage:

30 mg/kg
Administration:

s.c.; single dose
Result:

Seven days after a single 30 mg/kg s.c. dose, kidney miR-17 displacement miPSA score was 3.16, representing 89% inhibition.
Displacement began within 24 h, peaked at day 7, and continued for at least 14 days.

Animal Model:

C57BL/6 (JCK/C57BL6)^[3]
Dosage:

30 mg/kg
Administration:

s.c.; single dose
Result:

Seven days after a single 30 mg/kg s.c. dose, kidney miR-17 displacement miPSA score was 2.58, representing 83% inhibition.

Animal Model:

CD-1 (Pcy/CD1)^[3]
Dosage:

30 mg/kg
Administration:

s.c.; single dose
Result:

Seven days after a single 30 mg/kg s.c. dose, kidney miR-17 displacement miPSA score was 2.56, representing 83% inhibition.

Animal Model:

Pkhd1/cre;Pkd2F/F (Pkd2-KO)^[3]
Dosage:

20 mg/kg
Administration:

s.c.; postnatal days 10, 11, 12, and 19
Result:

Reversed the age-dependent decline in miR-17 PD-Sig, upregulated Pkd1 and Pkd2 expression, reduced kidney-to-body-weight ratio, and decreased cyst epithelial cell proliferation.
Kidney RNA-seq showed global de-repression of predicted miR-17 target genes and improved expression of 994 genes; Spearman rho = -0.559.

Animal Model:

CD-1 (Pcy/CD1)^[3]
Dosage:

25 mg/kg
Administration:

s.c.; QW or Q4W; 25 consecutive weeks; QW; 15 consecutive weeks (late intervention)
Result:

Weekly or monthly dosing reduced kidney-to-body-weight ratio, cyst index, urine Ngal protein, and kidney Ngal mRNA expression; late dosing did not attenuate cyst growth.
Kidney RNA-seq showed improved expression of 658 genes;.

Animal Model:

DBA/2 (Pcy/DBA)^[3]
Dosage:

1, 5 and 25 mg/kg (QW for 9 weeks); 25 mg/kg (Q4W for 9 weeks)
Administration:

s.c.; QW or Q4W; 9 consecutive weeks
Result:

Weekly dosing produced dose-dependent reductions in kidney-to-body-weight ratio and cyst index; monthly dosing did not confer efficacy.
Tolvaptan reduced kidney-to-body-weight ratio but did not improve cyst index.

Animal Model:

DBA/2 (Pcy/DBA)^[3]
Dosage:

30 mg/kg
Administration:

s.c.; QW; 8 consecutive weeks
Result:

bwTKV increased almost linearly in PBS control mice, whereas kidney growth plateaued after only 4 weeks of dosing; 1 of 10 mice receiving weekly dosing showed stabilization and 2 of 10 showed reduction of bwTKV.
MRI-based TKV showed a 50% reduction in bwTKV.

Chemical Information

CAS. Nr. 2229964-07-0
Appearance Solid
Molecular Weight 3082.42
Formel C₉₅H₁₁₅F₃N₃₂O₅₁P₈S₈
Color White to off-white
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
Synonyms

RG4326
Sequence

5’-AsGsCmAfCfUfUmUsGs-3‘
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

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

Publications (1)

All Bio/Physico-chemical AssayWB

Sort by:

Journal Impact Factor

Patent

US20250283086A1.

RGLS4326 purchased from MedChemExpress. Usage Cited in: Patent. US20250283086A1.

PC1 protein analysis in PPMO-treated WT9-7 cells. WT9-7 cells were incubated with PPMOs with the sequences corresponding to SEQ ID NO:47 (+604+628) in quadruplicate and a non-targeting control (NTC) for 2, 3 or 5 days. A non-targeting control (NTC) was used as a negative control and an inhibitor of miR-17 (RGLS4326), was included as a positive control.

RGLS4326 purchased from MedChemExpress. Usage Cited in: Patent. US20250283086A1.

Western blot images of PPMO-treated HEK293 cells. HEK293 cells were treated with PPMOs (+604+628) and (+611+635) with the sequences corresponding to SEQ ID NOs:47, and 334, respectively. A non-targeting control (NTC) was used as a negative control while an inhibitor of miR-17 (RGLS4326), was included as a positive control. PPMO-treated cells were harvested at 5 days and analysed for PC1 expression using western blot assay.

Lösungsmittel & Löslichkeit

In Vitro:

H₂O : ≥ 100 mg/mL (32.44 mM)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.3244 mL

1.6221 mL

3.2442 mL

5 mM

0.0649 mL

0.3244 mL

0.6488 mL

10 mM

0.0324 mL

0.1622 mL

0.3244 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (323 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2242 KB)

Verweise

[1]. Valencia T, et al. The nucleobase guanine at the 3'-terminus of oligonucleotide RGLS4326 drives off-target AMPAR inhibition and CNS toxicity. Nature communications. 2025 Nov 28;16(1):10762. [Content Brief]

[2]. Lakhia R, et al. PKD1 and PKD2 mRNA cis-inhibition drives polycystic kidney disease progression. Nature communications. 2022 Aug 15;13(1):4765.

[3]. Lee EC, et al. Discovery and preclinical evaluation of anti-miR-17 oligonucleotide RGLS4326 for the treatment of polycystic kidney disease. Nature communications. 2019 Sep 12;10(1):4148. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Bioz

RGLS4326

1 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

RGLS4326

Publications Citing Use of MedChemExpress (MCE) RGLS4326

Alle iGluR Isoform-spezifische Produkte anzeigen