RGLS4326(Synonyms: RG4326)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

RGLS4326 (Synonyms: RG4326)

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。

RGLS4326(Synonyms: RG4326)

RGLS4326 Chemical Structure

CAS No. : 2229964-07-0

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生物活性

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]
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 EC50 value of 77.2 ± 20.2 nM[1].
RGLS4326 suppresses the growth of primary human autosomal dominant polycystic kidney disease (ADPKD) cysts[1].

Shanghai Jinpan Biotech Co Ltd 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.

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 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].

Shanghai Jinpan Biotech Co Ltd 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.

分子量

3082.42

Formula

C95H115F3N32O51P8S8
CAS 号

2229964-07-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Edmund C Lee, et al. Discovery and preclinical evaluation of anti-miR-17 oligonucleotide RGLS4326 for the treatment of polycystic kidney disease. Nat Commun. 2019 Sep 12;10(1):4148.

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