产品名称

A-971432

一般描述

A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist

别称

1-(4-(3,4-Dichlorobenzyloxy)benzyl)azetidine-3-carboxylic acid

纯 度

≥95.0%(HPLC)

CAS NO.

1240308-45-5

分子式

C¹⁸H¹⁷Cl²NO³

分子量

366.24

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

白色至米色固体

溶解性(25℃)

DMSO

Slightly soluble

l  生物学信息

生物活性/药理作用

A-971432 is an orally bioavailable, non-clastogenic, azetidinecarboxylate compound that acts as a highly potent and selective sphingosine-1-phosphate receptor 5 agonist (IC50 = 6 nM/S1P5, 362 nM/S1P1 and >10 μM/S1P3 in a radio-ligand binding assay) without affect the activity of 129 protein kinases (IC50 >10 μM).  A-971432 is shown to enhance blood-brain barrier integrity and reverse lipid accumulation and age-related cognitive decline in mice in vivo with good pharmacokinetics (t1/2 = 5.7 h; Cmax = 2,500 ng/ml; AUC = 35,000 ng.h/ml at 10 mg/kg, p.o. in CD1 mice). Likewise, oral gavage showed good plasma exposure and no sign of lymphopenia in rats (10, 30, and  100 mg/kg.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.  https://www.ncbi.nlm.nih.gov