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3-Amino-1-propanesulfonic Acid
3-氨基-1-丙磺酸 /3-Amino-1-propanesulfonic Acid
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货号：A140624
同义名：
3-氨基丙烷磺酸;高牛黄酸
/ Tramiprosate;Homotaurine
3-Amino-1-propanesulfonic Acid 是一种可透过血脑屏障的天然氨基酸，通过靶向可溶性Aβ，减少淀粉样斑块沉积，并保持Aβ处于非纤维状形式，发挥神经保护，抗惊厥和抗高血压的作用。
3-Amino-1-propanesulfonic Acid 化学结构
3-Amino-1-propanesulfonic Acid 3D分子结构
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3-Amino-1-propanesulfonic Acid 纯度/质量文件 产品仅供科研
货号：A140624
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3-Amino-1-propanesulfonic Acid 质控信息
3-Amino-1-propanesulfonic Acid 生物活性
描述
Tramiprosate targets soluble Aβ, interacts with Aβ peptide and prevents its aggregation. Tramiprosate favours tau aggregation, in tau transfected non-neuronal cells, and in neuronal cells. It does not affect the binding of tau to microtubules but may prevent the formation of tau-actin aggregates[4] 42 -induced cell death in neuronal cell cultures, and to inhibit amyloid deposition. It can cross the murine blood-brain barrier (BBB) to exert its activity. Treatment of TgCRND8 mice with Tramiprosate resulted in significant reduction (∼30%) in the brain amyloid plaque load and a significant decrease in the cerebral levels of soluble and insoluble Aβ40 and Aβ42 (∼20–30%). Tramiprosate influenced the central pool of Aβ, changing either its efflux or its metabolism in the brain, as a reduction up to 60% of plasma Aβ levels was observed[5]
作用机制
Tramiprosate is a sulfated glycosaminoglycan mimetic which can interact with Aβ peptide, preventing its aggregation.[4]
3-Amino-1-propanesulfonic Acid 动物研究
Dose
Mice: 100 mg/kg, 500 mg/kg[3]
Administration
p.o.
Pharmacokinetics
Animal
Rats[3]
Dose
30 mg/kg (p.o.)
Administration
p.o.
F
~100% (p.o.)
AUC0-inf
19061 ng/ml·h (p.o.)
T1/2
4.4 h (p.o.)
Vz
43.6 l/kg (i.v.)
Tmax
0.5 h (p.o.)
CL
2.7 l/kg/h (i.v.)
Cmax
8943 ng/ml (p.o.)
Vss
12.9 l/kg (i.v.)
AUC0→t
18894 ng/ml·h (p.o.)
3-Amino-1-propanesulfonic Acid 参考文献
[1] Santa-Maria I, Hernández F, et al. Tramiprosate, a drug of potential interest for the treatment of Alzheimer's disease, promotes an abnormal aggregation of tau. Mol Neurodegener. 2007 Sep 6;2:17.
[2] Gervais F, Paquette J, et al. Targeting soluble Abeta peptide with Tramiprosate for the treatment of brain amyloidosis. Neurobiol Aging. 2007 Apr;28(4):537-47. Epub 2006 May 3.
[3] Hey JA, Yu JY, et al. Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimer's Disease. Clin Pharmacokinet. 2018 Mar;57(3):315-333.
[4] Santa-Maria I, Hernández F, Del Rio J, Moreno FJ, Avila J. Tramiprosate, a drug of potential interest for the treatment of Alzheimer's disease, promotes an abnormal aggregation of tau. Mol Neurodegener. 2007 Sep 6;2:17. doi: 10.1186/1750-1326-2-17. PMID: 17822548; PMCID: PMC2048960.
[5] Gervais F, Paquette J, Morissette C, Krzywkowski P, Yu M, Azzi M, Lacombe D, Kong X, Aman A, Laurin J, Szarek WA, Tremblay P. Targeting soluble Abeta peptide with Tramiprosate for the treatment of brain amyloidosis. Neurobiol Aging. 2007 Apr;28(4):537-47. doi: 10.1016/j.neurobiolaging.2006.02.015. Epub 2006 May 3. PMID: 16675063.
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3-Amino-1-propanesulfonic Acid 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
7.19mL
1.44mL
0.72mL
35.93mL
7.19mL
3.59mL
71.85mL
14.37mL
7.19mL
3-Amino-1-propanesulfonic Acid 技术信息
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