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CID 1375606

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Chemical Structure| 313493-80-0 同义名 : -
CAS号 : 313493-80-0
货号 : A934025
分子式 : C20H14Cl2N2O2
纯度 : 99%+
分子量 : 385.243
MDL号 : MFCD00369571
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(129.79 mM)，配合低频超声助溶，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 GPR27, belonging to G protein-coupled receptors (GPCR), is an orphan receptor which remains devoid of confirmed ligand and has recently been linked to insulin secretion. CID 1375606 is a surrogate agonist of GPR27 which is selective for GPR27 over its closely related family members GPR85 and GPR173. CID 1375606 displayed potent efficacy on GPR27V2 with pEC50 value of 6.34 ± 0.13 in the firefly luciferase complementation assay. Furthermore, there was a formation of small endosome-like clusters near the membrane in the presence of CID 1375606 (50 μM) and the receptor GPR27V2 in living cells confirming the β-arrestin 2 recruitment ability of CID 1375606. In an alternative assay based on β-galactosidase complementation upon recruitment of β-arrestin 2 to GPR27 in CHO-K1 cells, CID 1375606 concentration-dependently increased the signal with pEC50 of 5.3 ± 0.03[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.60mL

0.52mL

0.26mL

12.98mL

2.60mL

1.30mL

25.96mL

5.19mL

2.60mL
参考文献

[1]Dupuis N, Laschet C, Franssen D, Szpakowska M, Gilissen J, Geubelle P, Soni A, Parent AS, Pirotte B, Chevigné A, Twizere JC, Hanson J. Activation of the Orphan G Protein-Coupled Receptor GPR27 by Surrogate Ligands Promotes β-Arrestin 2 Recruitment. Mol Pharmacol. 2017 Jun;91(6):595-608