A-971432
目录号 : KCM10781 CAS No. : 1240308-45-5 纯度 : ≥98%
A-971432 is a sphingosine-1-phosphate receptor 5 (S1P) agonist that is selective for S1P over S1P and S1P (ICs = 0.006, 0.362, and >10 µM, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P (EC = 4.1 nM). A-971432 (1 µM) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington's disease when administered at a dose of 0.1 mg/kg. A-971432 (0.1 mg/kg per day, i.p.) decreases the number of errors made in a horizontal ladder task and increases latency to fall in the rotarod test in R6/2 mice. It also increases spontaneous alternation in the t-maze in aged mice when administered at a dose of 0.1 mg/kg.
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1mg
In-stock
5mg
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10mg
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25mg
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生物活性

A-971432 is a potent, selective and orally active sphingosine-1-phosphate (S1P) receptor 5 agonist with IC50s of .362, >10, 0.006 μM for S1P1, S1P3, S1P5 respectively. A-971432 protects blood–brain barrier (BBB) homeostasis. A-971432 reverses age-related cognitive decline. A-971432 has the potential for the research of alzheimer’s disease or multiple sclerosis.

体外研究

A-971432 (0-10 μM) shows selectivity with IC50s of 0.362, >10, 0.006 μM for S1P1, S1P3, S1P5 respectively.

A-971432 (0.1-1000 nM) induces full agonism with an EC50s of 5.7 nM and 4.1 nM for HEK cells and CHO cells, respectively.

分子式
C18H17Cl2NO3
分子量
366.23792
CAS号
1240308-45-5
中文名称
1-({4-[(3,4-dichlorophenyl)methoxy]phenyl}methyl)azetidine-3-carboxylic acid
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据
In Vitro: 

DMSO: 2.5 mg/mL (6.83 mM; ultrasonic and warming and heat to 60°C)

配制储备液
                                           
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
                                                                                                                    
1 mM 2.7304 mL 13.6523 mL 27.3045 mL
5 mM 0.5461 mL 2.7304 mL 5.4609 mL
10 mM --- --- ---
*

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, 6 months; -20°C, 1 month。-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。

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