|2,4-二氯-N-(4-苯基氨基甲酰基)苯基)苯甲酰胺|CsnPharm

CAS No.: 313493-80-0

CID 1375606 Catalog No. CSN23236

Synonyms: 2;4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide

CID 1375606 is an agonist of GPR27 (SREB1) that induces coupling of the receptor to β-arrestin 2.

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技术信息

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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5958 mL
- 12.9788 mL
- 25.9576 mL
- 5 mM
- 0.5192 mL
- 2.5958 mL
- 5.1915 mL
- 10 mM
- 0.2596 mL
- 1.2979 mL
- 2.5958 mL

技术信息

CAS号

313493-80-0

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H14Cl2N2O2

运输

蓝冰

分子量

385.24

别名

2;4-Dichloro-N-(phenylcarbamoyl)phenylbenzamide

溶解度

DMSO	50.0 mg/mL (129.8 mM)
Water	insoluble

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