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.
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 : 93.56%
- CAS 番号: 2921918-19-4
- 分子式: C95H107F3N32Na8O50P8S8
- 分子量:3066.4 (free acid)
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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
製品説明
体外実験
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.
体内実験
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.
化学情報
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CAS 番号 2921918-19-4
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性状 Solid
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分子量 3066.4 (free acid)
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分子式 C95H107F3N32Na8O50P8S8
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Color White to off-white
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SMILES
[Farabursen (sodium)]
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別名
RGLS8429 sodium; RG1015 sodium
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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 (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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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)