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.
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- CAS. Nr.: 1404506-35-9
- Formel: C21H19ClN4O
- Molecular Weight:378.85
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1404506-35-9
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Molecular Weight 378.85
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BF844 Related Classifications
HY-120726 Related Classifications
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