Farabursen sodium
Based on 1 Customer Validation
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.
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- Pureza : 93.56%
- No. CAS: 2921918-19-4
- Fòrmula: C95H107F3N32Na8O50P8S8
- Peso molecular:3066.4 (free acid)
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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- Pureza y Documentación
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Help & FAQs
Actividad biológica
Descripciòn
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. Further protocols information, click here.
In Vivo
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.
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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]
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Dosage:20 mg/kg
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Administration:s.c.; on postnatal days 8, 10, 12, 15
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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.
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Animal Model:C57BL/6 mice[2]
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Dosage:03, 0.03, 0.1, 0.3, 1, 3, 10, 30, and 300 mg/kg
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Administration:s.c.; single dose
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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.
Chemical Information
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No. CAS 2921918-19-4
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Appearance Solid
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Peso molecular 3066.4 (free acid)
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Fòrmula C95H107F3N32Na8O50P8S8
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Color White to off-white
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SMILES
[Farabursen (sodium)]
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Synonyms
RGLS8429 sodium; RG1015 sodium
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Protocolo
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Ki-67 Immunostaining Proliferation Assay
Ki-67 immunostaining measures the growth fraction of a cell population by detecting Ki-67, a nuclear antigen present in proliferating cells and absent in quiescent G0 cells. The readout is the percentage of Ki-67-positive nuclei among total counted cells, commonly called the Ki-67 labeling index or proliferation index.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (270 KB)
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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)
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Instrucciones de manejo (2242 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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