产品
编 号:F741059
分子式:C28H27F4N3O4S
分子量:577.59
产品类型
结构图
CAS No: 924759-42-2
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生物活性:
BT44 is a selective RET activator. BT44 can penetrate through the blood-brain barrier and can be used for the research of neurodegenerative disorders and diabetes mellitus.
体内研究:
BT44 (5-25 mg/kg; s.c.; every second day for 10, 42 or 14 days) 在神经性的 SNL 和 STZ 模型中可减轻感觉体征。BT44 (12.5 or 25 mg/kg; s.c.; every second day for 10 days) 对实验性神经病变动物 DRGs 中 IB4 阳性神经元有保护作用。BT44 (0.1 and 0.3 μg/24 h; infuse into the right dorsal striatum for 14 days) 在 6-OHDA 帕金森大鼠模型中逆转 amphetamine 引起的运动失衡,似乎保护纹状体中的多巴胺能纤维。BT44 (10 mg/kg; i.v.) 穿过血脑屏障,在大鼠中迅速从循环 (半衰期 (t1/2) = 0.72 h) 和脑 (t1/2 = 0.47 h) 中消除。Animal Model:Wistar rats, spinal nerve ligation (SNL) and Streptozotocin (STZ; HY-13753)-induced diabetes mellitus models
Dosage:5, 12.5 or 25 mg/kg
Administration:Subcutaneous injecton, every second day for 10, 42 or 14 days
Result:Alleviated mechanical allodynia in the SNL animals. Treatment with the dose of 5 mg/kg alleviated mechanical hyperalgesia in the STZ-treated animals, while the 12.5 mg/kg dose was not effective. Concentration of 5 mg/kg attenuated cold allodynia in the STZ-treated animals during the first two weeks while the effect of 12.5 mg/kg was not significant.
Animal Model:Wistar rats, SNL-induced diabetes mellitus model
Dosage:12.5 or 25 mg/kg
Administration:Subcutaneous injecton, every second day for 10 days
Result:Led to a significant increase in the number of IB4 expressing neurons in the ipsilateral DRGs. The 12.5 mg/kg dose protected IB4-positive neurons from SNL-induced lesion.
体外研究:
BT44 (7.5-75 μM; 15 min) 促进 RET 磷酸化并选择性激活表达 GFL 受体的细胞的下游级联反应。BT44 (0.5-10 μM; 16-20 h) 促进感觉神经元的神经突生长。