TrkB Agonist Prodrug R13
(Synonyms: TrkB-IN-1; Tropomyosin-related Kinase B Agonist Prodrug R13; Tropomyosin-related Kinase B Inhibitor 1) 目录号 : GC91977TrkB Agonist Prodrug R13（R13）是原肌球蛋白相关激酶B（TrkB）激活剂7,8-二羟基黄酮的前药形式。
Cas No.:1609067-49-3
Sample solution is provided at 25 µL, 10mM.
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TrkB agonist prodrug R13 (R13) is a prodrug form of the tropomyosin-related kinase B (TrkB) activator 7,8-dihydroxyflavone.1 Oral administration of R13 (43.6 mg/kg per day) increases hippocampal phosphorylated levels of TrkB, ERK, and Akt in the 5XFAD transgenic mouse model of Alzheimer's disease. It decreases the number of malformed neurons and increases the number of neurons and active synapses in the hippocampus in 5XFAD mice. R13 decreases the number of plaques and levels of amyloid-β (1-40) (Aβ40) in the hippocampus and frontal cortex and escape latency in the Morris water maze in 5XFAD mice. It reduces the levels and activity of δ-secretase, also known as asparagine endopeptidase (Aep) and legumain, and the levels of Il-6, Tnf-α, and Il-1β in brain homogenates from 5XFAD mice.
References:
[1]. Chen, C., Wang, Z., Zhang, Z., et al.The prodrug of 7,8-dihydroxyflavone development and therapeutic efficacy for treating Alzheimer's diseaseProc. Natl. Acad. Sci. U S A115(3)578-583(2018).
| Cas No. | 1609067-49-3 | SDF | |
| 别名 | TrkB-IN-1; Tropomyosin-related Kinase B Agonist Prodrug R13; Tropomyosin-related Kinase B Inhibitor 1 | ||
| 化学名 | 7,8-bis[[(methylamino)carbonyl]oxy]-2-phenyl-4H-1-benzopyran-4-one | ||
| Canonical SMILES | O=C(NC)OC1=C(OC(C2=CC=CC=C2)=CC3=O)C3=CC=C1OC(NC)=O | ||
| 分子式 | C19H16N2O6 | 分子量 | 368.3 |
| 溶解度 | Acetonitrile: Slightly soluble: 0.1-1 mg/ml,DMSO: Slightly soluble: 0.1-1 mg/ml,Water: Slightly soluble: 0.1-1 mg/ml | 储存条件 | -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7152 mL | 13.5759 mL | 27.1518 mL |
| 5 mM | 0.543 mL | 2.7152 mL | 5.4304 mL |
| 10 mM | 0.2715 mL | 1.3576 mL | 2.7152 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet