BF844
BF844 mitigate hearing loss associated with USH3 (usher syndrome type III) mutation CLRN1 (clarin-1)N48K. BF844 induces CLRN1N48K transportes to the plasma membrane. BF844 shows significantly preserves hearing in vivo.
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。
- CAS 番号: 1404506-35-9
- 分子式: C21H19ClN4O
- 分子量:378.85
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
BF844 (compound 3) (0.846 μM) effectively inhibits HSP60 activity (87.07±27.70% inhibition) and moderately inhibited HSP90 (40.06±19.10% inhibition)[1].
BF844 (2.90 μM; 24 h) induces about 6% of total CLRN1N48K to be transported to the plasma membrane in C1, D1, D6 cells[1].
BF844 (2.90 μM; 24 h) effectively increases the amount of non-glycosylated CLRN1 and non-glycosylated CLRN1 is effectively transported to the plasma membrane in C1 and D1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
BF844 (10 mg/kg; i.p.) shows significantly preserves hearing in Tg;KI/KI mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Juvenile mice[1]
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Dosage:3, 10 mg/kg (3 mg/kg for P6 (post-natal day 6) mice, 10 mg/kg for P20 (post-natal day 20) mice)
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Administration:I.p.
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Result:Showed AUC values were determined to be 1.76 μM.h and 1.98 μM.h.
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Animal Model:P30 Tg;KI/KI C57BL/6J mice[1]
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Dosage:30 mg/kg
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Administration:I.p.; daily from P30 to P45
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Result:Showed significantly preserves hearing with the median threshold of sound intensity in log scale was 57.5–67.5 dB SPL and about 1,000 times more sensitive hearing compared to untreated controls at P55.
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Animal Model:P10 Tg;KI/KI C57BL/6J mice[1]
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Dosage:10 mg/kg
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Administration:I.p.; 10 mg/kg every other day and gradually escalated the dose up to 20 mg/kg at P28. From P30 to P45, mice received 30 mg/kg daily
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Result:Showd the median threshold of sound intensity in log scale was 55, 42.5 and 37.5 dB SPL lower at 8, 16 and 32 kHz at P55, respectively.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1404506-35-9
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分子量 378.85
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分子式 C21H19ClN4O
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SMILES
CC(O)(C)CN1N=C(C2=CC=CC=C2)C3=C(Cl)C(C4=CC=CC=C4)=NN=C31
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
BF844 関連分類
HY-120726 関連分類
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