1. Epigenetics
  2. MicroRNA
  3. Farabursen sodium

Farabursen sodium  (Synonyms: RGLS8429 sodium; RG1015 sodium)

Cat. No.: HY-150364A Purity: 93.56%
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Farabursen sodium (RGLS8429 sodium; RG1015 sodium) is a miR-17 inhibitor. Farabursen sodium inhibits the function of the miR-17 family, relieves the inhibitory effect on miR-17 target genes including PKD1 and PKD2, and increases the level of PC1/2. Farabursen sodium slows the growth of renal cysts, reduces the ratio of kidney weight to body weight, and decreases the cyst index and proliferation index. Farabursen sodium is applicable to research related to autosomal dominant polycystic kidney disease.

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

RNA, (P-thio)([2',5'-anhydro-6'-deoxy-4'-C-(hydroxymethyl)-α-L-mannofurano]A-(3'→4')-[2',5'-anhydro-6'-deoxy-4'-C-(hydroxymethyl)-α-L-mannofurano]G-Cm-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'-fluoro)C-(2'-deoxy-2'-fluoro)U-Um-(3'→4')-[2',5'-anhydro-6'-deoxy-4'-C-(hydroxymethyl)-α-L-mannofurano]U-(3'→4')-[2',5'-anhydro-6'-deoxy-4'-C-(hydroxymethyl)-α-L-mannofurano]A), sodium salt (1:8)

Farabursen sodium Chemical Structure

CAS No. : 2921918-19-4

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Description

Farabursen sodium (RGLS8429 sodium; RG1015 sodium) is a miR-17 inhibitor. Farabursen sodium inhibits the function of the miR-17 family, relieves the inhibitory effect on miR-17 target genes including PKD1 and PKD2, and increases the level of PC1/2. Farabursen sodium slows the growth of renal cysts, reduces the ratio of kidney weight to body weight, and decreases the cyst index and proliferation index. Farabursen sodium is applicable to research related to autosomal dominant polycystic kidney disease[1][2].

In Vitro

Farabursen (sodium) (0.1-100 nM; 24 h) potently de-represses miR-17 activity in HeLa cells, with an EC50 of 22.40 nM after 24 h of incubation[2].
Farabursen (sodium) (0.1-100 nM; 24 h) de-represses PKD1-3'UTR activity in HeLa cells, with an EC50 of 43.54 nM after 24 h of incubation[2].
Farabursen (sodium) (0.1-100 nM; 24 h) de-represses PKD2-3'UTR activity in HeLa cells, with an EC50 of 40.76 nM after 24 h of incubation[2].
Farabursen (sodium) (120 nM) reduces 3D cyst size in primary human ADPKD cyst cells when transfected at 120 nM[2].

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

In Vivo

Farabursen sodium (20 mg/kg, s.c., administered on postnatal days 8, 10, 12, and 15) significantly inhibits renal cyst growth and cell proliferation, and improves renal function in Pkd1F/RC ADPKD mice[2].
Farabursen sodium (0-300 mg/kg; s.c.; single dose) achieves sustained target binding to miR-17 in the kidneys of C57BL/6 mice (inhibition rate ≥75%, duration ≥14 days), and also achieves this effect in the liver (inhibition rate ≥75%, duration ≥7 days), with an EC75 of 2.2 μg/g in renal tissues[2].

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

Animal Model: C57BL/6 mice (Pkd1F/RC genetic model of ADPKD; treated on postnatal days 8, 10, 12, 15, sacrificed on postnatal day 18)[2]
Dosage: 20 mg/kg
Administration: s.c.; on postnatal days 8, 10, 12, 15
Result: Reduced kidney weight-to-body weight (KW/BW) ratio, cyst index, proliferation index, and blood urea nitrogen (BUN) levels compared to PBS control; all reductions were statistically significant.
Animal Model: C57BL/6 mice[2]
Dosage: 03, 0.03, 0.1, 0.3, 1, 3, 10, 30, and 300 mg/kg
Administration: s.c.; single dose
Result: Achieved kidney target engagement (percent inhibition of miR-17) ≥75% for at least 14 days post-dose.
Achieved liver target engagement ≥75% for at least 7 days post-dose.
Reached an EC75 (kidney concentration required to achieve 75% target engagement) of 2.2 μg/g.
Molecular Weight

3066.4 (free acid)

Formula

C95H107F3N32Na8O50P8S8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[Farabursen (sodium)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: 93.56%

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  • 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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