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RGLS4326
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:2229964-07-0
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议

产品名称
RG4326
产品介绍
RGLS4326 (RG4326) 是一种首创的microRNA-17(miR-17) 寡核苷酸抑制剂。RGLS4326 可用于常染色体显性多囊肾病 (ADPKD) 的研究。RGLS4326 作用于 HeLa 细胞,抑制 miR-17 功能,EC50值为 28.3 nM。
生物活性

RGLS4326 (RG4326) is a first-in-class, short oligonucleotide inhibitor ofmicroRNA-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 EC50value of 28.3 nM[1].

IC50& Target

MicroRNA[1]

体外研究
(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 EC50value 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.
体内研究
(In Vivo)

RGLS4326 preferentially distributes to kidney tubules and cysts. RGLS4326 (a single 30 mg/kg SC injection) is rapidly absorbed into plasma, showing Tmaxof ≤1 h, Cmaxof 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 genesPkd1andPkd2[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-treatedPkd2-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
分子量

3082.42

性状

Solid

Formula

C95H115F3N32O51P8S8

CAS 号

2229964-07-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

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