产品介绍 |
BT44 是选择性 RET 活化剂。BT44 可穿透血脑屏障,可用于研究神经退行性疾病及糖尿病。
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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.
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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。
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line: |
GFRα3-transfected MG87RET cells |
Concentration: |
7.5, 18, 35 and 75 μM |
Incubation Time: |
15 min |
Result: |
Increased RET and ERK phosphorylation. |
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体内研究 (In Vivo) |
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。
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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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。
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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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。
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
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. |
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性状 | Solid |
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溶解性数据 |
In Vitro:
DMSO : 62.5 mg/mL (108.21 mM; ultrasonic and warming and heat to 60°C)
配制储备液
浓度
溶剂体积
质量
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1 mg |
5 mg |
10 mg |
1 mM |
1.7313 mL |
8.6567 mL |
17.3133 mL |
5 mM |
0.3463 mL |
1.7313 mL |
3.4627 mL |
10 mM |
0.1731 mL |
0.8657 mL |
1.7313 mL |
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Powder |
-20°C |
3 years |
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4°C |
2 years |
In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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参考文献 | |
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