Farabursen
Based on 1 Customer Validation
Farabursen (RGLS8429; RG1015) is a blood-brain barrier-permeable miR-17 inhibitor. Farabursen derepresses Pkd1 and Pkd2, the target genes of miR-17, increases the levels of PC1 and PC2, and reduces cyst growth. Farabursen decreases renal cyst growth, kidney weight-to-body weight ratio, cyst index, proliferation index, and blood urea nitrogen levels in mouse models. Farabursen is applicable to research related to autosomal dominant polycystic kidney disease.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.74%
- CAS 番号: 2953012-32-1
- 分子量:3066.36
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
Farabursen (0-3 μM; 30 s preincubation) exhibits only weak inhibitory activity against human GluA1/GluA4 AMPAR in HEK293 cells, with an inhibition rate of approximately 40% at the concentration of 3 μM[2].
Farabursen (0.1-100 nM; 24 h) potently inhibits the activity of miR-17 in HeLa cells with an EC50 of 22.4 nM, relieves the expression inhibition of miR-17 target gene PKD1 with an EC50 of 43.54 nM, and relieves the expression inhibition of miR-17 target gene PKD2 with an EC50 of 40.76 nM[2].
Farabursen (300 nM; 24-72 h) derepresses the expression of *Pkd1* and *Pkd2* genes, and increases the protein levels of PC1 and PC2 in mouse Pkd1RC/- ADPKD cells[2].
Farabursen (120 nM; 72 h post-transfection) increases the protein levels of PC1 and PC2, and inhibits cyst growth in primary human ADPKD cyst cells with the PKD1+/02641 genotype[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse Pkd1^RC/- ADPKD cells
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Concentration:300 nM
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Incubation Time:24 h post-transfection (gene expression analysis); 72 h post-transfection (protein levels analysis)
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Result:Significantly de-repressed Pkd1 and Pkd2 gene expression with fold changes of ~0.6760 and ~0.9286, respectively.
Increased PC1 and PC2 protein levels.
Farabursen (20 mg/kg; subcutaneous injection; postnatal days 8-15) reduces cyst growth, kidney enlargement, cell proliferation, and renal function decline in Pkd1F/RC ADPKD mice[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[2]
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Dosage:30 mg/kg
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Administration:s.c.; single dose
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Result:Showed a pharmacokinetic profile characterized by rapid absorption, rapid clearance, and preferential distribution to the kidney (kidney AUC_last exceeded liver AUC_last by >20-fold).
Reached ≥75% target engagement (percent inhibition of miR-17) in kidney tissue, which was maintained for 14 days; target engagement in liver tissue was ≤75% by 7 days.
Achieved a kidney EC75 (concentration corresponding to 75% miR-17 inhibition) of 2.2 μg/g.
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Animal Model:Ksp/Cre; Pkd1F/RC (autosomal dominant polycystic kidney disease model)[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 ratio, cyst index, proliferation index, and blood urea nitrogen (BUN) levels.
化学情報
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CAS 番号 2953012-32-1
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性状 Solid
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分子量 3066.36
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Color White to off-white
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SMILES
[Farabursen]
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別名
RGLS8429; RG1015
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (252 KB)
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- 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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取扱説明書 (2242 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)