|3-氨基-1-丙烷磺酸|CsnPharm

CAS No.: 3687-18-1

3-Amino-1-propanesulfonic Acid/3-氨基-1-丙磺酸 Catalog No. CSN13757

Synonyms: Homotaurine;3-Amino-1-propanesulfonic acid;Alzhemed

Tramiprosate targets soluble Aβ to decrease amyloid plaque deposition and maintains Aβ in a non-fibrillar form.

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实验方案

技术信息

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]. Tramiprosate was found to maintain Aβ in a non-fibrillar form, to decrease Aβ₄₂-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]

动物研究

剂量

Mice: 100 mg/kg, 500 mg/kg^[3] (p.o.)

给药途径

p.o.

动物药代数据

Animal	Rats^[3]
Dose	30 mg/kg (p.o.) 10 mg/kg (i.v.)
Administration	p.o. i.v.
F	~100% (p.o.)
AUC_0-inf	19061 ng/ml·h (p.o.) 3638 ng/ml·h (i.v.)
T_1/2	4.4 h (p.o.) 11.0 h (i.v.)
V_z	43.6 l/kg (i.v.)
T_max	0.5 h (p.o.) 0.083 h (i.v.)
CL	2.7 l/kg/h (i.v.)
C_max	8943 ng/ml (p.o.) 7484 ng/ml (i.v.)
Vss	12.9 l/kg (i.v.)
AUC_0→t	18894 ng/ml·h (p.o.) 3407 ng/ml·h (i.v.)

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00314912	Alzheimer's Disease	Phase 3	Unknown	-	United States, California ... more >> San Francisco Clinical Research Center San Francisco, California, United States Collapse <<
NCT00088673	Alzheimer Disease	Phase 3	Unknown	-	-
NCT00217763	Alzheimer's Disease	Phase 3	Unknown	December 2007	-

更多
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 7.1855 mL
- 35.9273 mL
- 71.8546 mL
- 5 mM
- 1.4371 mL
- 7.1855 mL
- 14.3709 mL
- 10 mM
- 0.7185 mL
- 3.5927 mL
- 7.1855 mL

技术信息

CAS号

3687-18-1

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C3H9NO3S

运输

蓝冰

分子量

139.17

别名

Homotaurine;3-Amino-1-propanesulfonic acid;Alzhemed;3-APS;NC 531;NSC 77071;3-Sulfopropylamine;NC-758;3-氨基丙烷磺酸;曲米前列酸

溶解度

DMSO	1.0 mg/mL (7.2 mM) warming
Water	20.0 mg/mL (143.7 mM) warming

动物实验配方

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3-Amino-1-propanesulfonic Acid/3-氨基-1-丙磺酸 Catalog No. CSN13757

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