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编 号:F029635
分子式:C32H31N3O5
分子量:537.61
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50μg
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100μg
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生物活性:
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+ concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases.

体内研究:
KT5720 (5 mg/kg;腹腔注射;每天一次,持续 8 天) 完全逆转 MDR1 转基因小鼠模型中的 DNR 耐药性。Animal Model:MDR1 transgenic mice model.
Dosage:5 mg/kg
Administration:Intraperitoneal injection; single daily for 8 days
Result:Exhibited the leukopenia induced by daunorubicin in the MDR mice was equivalent to that measured in non-MDR mice treated with daunorubicin alone.

体外研究:
KT5720 (0-8 μM;72 h) 在 MDR1 淋巴瘤细胞模型中逆转多药耐药性。 KT5720 (3 μM) 减弱 Ih 在新鲜分离的大鼠 DRG 神经元并减缓 HCN 通道激活动力学。 KT5720 (3 μM) 降低 DRG 神经元的兴奋性并降低 DRG 神经元细胞内 Ca2 +。
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