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Chemical Structure| 1206123-37-6 同义名 : APD334
CAS号 : 1206123-37-6
货号 : A107759
分子式 : C26H26F3NO3
纯度 : 99%+
分子量 : 457.48
MDL号 : MFCD28502134
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(65.58 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 APD334 is a newly designed, highly specific antagonist targeting S1P1 receptors. In CHO cells expressing HA-tagged S1P1 receptors, APD334 demonstrates an IC50 value of 1.88 nM. While showing some degree of activation at human S1P4 and S1P5 receptors, this activation is notably weaker compared to S1P1, both in terms of potency and efficacy. Notably, APD334 does not exhibit any agonistic or antagonistic effects on human S1P2 and S1P3 receptors. Pharmacokinetic studies across various preclinical species demonstrate favorable central exposure and a promising pharmacokinetic profile. S1P1 receptor activity is maintained in mice (EC50=0.44 nM), rats (EC50=0.32 nM), dogs (EC50=0.34 nM), and monkeys (EC50=0.32 nM) [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.93mL

2.19mL

1.09mL

21.86mL

4.37mL

2.19mL
参考文献

[1]Buzard DJ, et al. Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. ACS Med Chem Lett. 2014 Nov 4;5(12):1313-7.