Valiltramiprosate (Synonyms: ALZ-801)
目录号: PL13284 纯度: ≥98%
CAS No. :1034190-08-3
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中文名称
Valiltramiprosate
中文别名
3-[[(2S)-2-氨基-3-甲基-1-氧代丁基]氨基]-1-丙烷磺酸
英文名称
Valiltramiprosate
英文别名
(S)-3-(2-aMino-3-MethylbutanaMido)propane-1-sulfonic acid;3-[(2S)-2-amino-3-methylbutanamido]propane-1-sulfonic acid;ALZ 801;ALZ-801;NRZRFNYKMSAZBI-ZETCQYMHSA-N;Valiltramiprosate
Cas No.
1034190-08-3
分子式
C8H18N2O4S
分子量
238.30
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
ALZ-801 是一种口服可用的小分子 β-淀粉样蛋白 β-amyloid (Aβ) 抑制剂, Tramiprosate 缬氨酸偶联前药,有显著改善的 PK 特性和胃肠耐受性。ALZ-801 有潜力用于研究阿尔茨海默病的研究。
生物活性
ALZ-801 is a potent and orally available small-molecule β-amyloid (Aβ) anti-oligomer and aggregation inhibitor, valine-conjugated prodrug of Tramiprosate with substantially improved PK properties and gastrointestinal tolerability compared with the parent compound. ALZ-801 is an advanced and markedly improved candidate for the treatment of alzheimer’s disease.
性状
Solid
IC50 & Target[1][2]
β-amyloid
体内研究(In Vivo)
ALZ-801 (oral administration; 172 mg/kg; single dose) exhibits mean AUCt values of 58,758 and 5841 ng/ml.h in plasma and brain, respectively. The ALZ-801: Tramiprosate ratio in plasma and brain is 1.8 and 3.1, respectively in male CD-1 mice.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
ClinicalTrial
参考文献
[1]. John A. Hey, et al. Discovery and Identification of an Endogenous Metabolite of Tramiprosate and Its Prodrug ALZ-801 that Inhibits Beta Amyloid Oligomer Formation in the Human Brain. CNS Drugs. 2018; 32(9): 849–861.
[2]. Hey JA, et al. Clinical Pharmacokinetics and Safety of ALZ-801, a Novel Prodrug of Tramiprosate in Development for the Treatment of Alzheimers Disease. Clin Pharmacokinet. 2018 Mar;57(3):315-333.
溶解度数据
In Vitro: H2O : 30 mg/mL (125.89 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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