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编 号：F152161
分子式：C21H19ClN4O
分子量：378.85
分子式：C21H19ClN4O
分子量：378.85
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CAS No: 1404506-35-9
产品详情
生物活性：
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.
体内研究：
BF844 shows good penetration into the retina and cochlea in vivo.BF844 (10 mg/kg; i.p.) shows significantly preserves hearing in Tg;KI/KI mice.Animal Model:Juvenile mice
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)
Administration:I.p.
Result:Showed AUC values were determined to be 1.76 μM.h and 1.98 μM.h.
Animal Model:P30 Tg;KI/KI C57BL/6J mice
Dosage:30 mg/kg
Administration:I.p.; daily from P30 to P45
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.
Animal Model:P10 Tg;KI/KI C57BL/6J mice
Dosage:10 mg/kg
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
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.
体外研究：
BF844 (compound 3) (0.846 μM) effectively inhibits HSP60 activity (87.07±27.70% inhibition) and moderately inhibited HSP90 (40.06±19.10% inhibition).BF844 (2.90 μM; 24 h) induces about 6% of total CLRN1N48K to be transported to the plasma membrane in C1, D1, D6 cells.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.
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.
体内研究：
BF844 shows good penetration into the retina and cochlea in vivo.BF844 (10 mg/kg; i.p.) shows significantly preserves hearing in Tg;KI/KI mice.Animal Model:Juvenile mice
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)
Administration:I.p.
Result:Showed AUC values were determined to be 1.76 μM.h and 1.98 μM.h.
Animal Model:P30 Tg;KI/KI C57BL/6J mice
Dosage:30 mg/kg
Administration:I.p.; daily from P30 to P45
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.
Animal Model:P10 Tg;KI/KI C57BL/6J mice
Dosage:10 mg/kg
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
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.
体外研究：
BF844 (compound 3) (0.846 μM) effectively inhibits HSP60 activity (87.07±27.70% inhibition) and moderately inhibited HSP90 (40.06±19.10% inhibition).BF844 (2.90 μM; 24 h) induces about 6% of total CLRN1N48K to be transported to the plasma membrane in C1, D1, D6 cells.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.
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