AF64394

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Chemical Structure| 1637300-25-4 同义名 : -
CAS号 : 1637300-25-4
货号 : A935740
分子式 : C21H20ClN5O
纯度 : 98%+
分子量 : 393.87
MDL号 : MFCD28411712
存储条件：

Pure form Sealed in dry, 2-8°C

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

DMSO: 120 mg/mL(304.67 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
生物活性
描述 GPR3 is orphan G-protein coupled receptor (GPCR) which results in elevated levels of cellular cAMP when overexpressing in heterologous expression systems as well as in primary neurons. AF64394 is a novel and selective GPR3 inverse agonist with pIC50 value of 7.3, 5.1 and 4.9 for GPR3, GPR6 and GPR12, respectively. AF34394 is specific and selective and thus forms useful tool for delineating the biology of GPR3. Whilst AF34394 is only of modest potency and relatively lipophilic (clogP = 5.2, LLE = 2.1), it shows promising SAR (structure activity relationship) and represents an excellent start point for further optimisation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.54mL

0.51mL

0.25mL

12.69mL

2.54mL

1.27mL

25.39mL

5.08mL

2.54mL
参考文献

[1]Jensen T, Elster L, Nielsen SM, Poda SB, Loechel F, Volbracht C, Klewe IV, David L, Watson SP. The identification of GPR3 inverse agonist AF64394; the first small molecule inhibitor of GPR3 receptor function. Bioorg Med Chem Lett. 2014 Nov 15;24(22):5195-8