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Chemical Structure| 1621175-65-2 同义名 : GPR39-C3
CAS号 : 1621175-65-2
货号 : A724127
分子式 : C18H19ClN6O2S
纯度 : 98%+
分子量 : 418.901
MDL号 : MFCD30182283
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: 105 mg/mL(250.66 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 GPR39 is a putative zinc-sensing G protein-coupled receptor (GPCR) related to the ghrelin/neurotensin peptide receptor subfamily which is implicated in cellular processes such as insulin secretion, protection from cell death, gastric emptying, and epithelial repair. GPR39-C3 is a potent and oral active GPR39 agonist with EC50s of 0.4 and 0.8 nM for rat and human receptors, respectively[1]. As a GPR39 positive allosteric modulator, GPR39-C3 activated cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment in HEK293-GPR39 cells. Moreover, GPR39-C3 induced dose- and time-dependent loss of response in cAMP production by second challenge of the compound[2]. In vivo, GPR39-C3 (30 mg/kg po) robustly induced acute GLP-1 levels in mice which is a PD marker[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.39mL

0.48mL

0.24mL

11.94mL

2.39mL

1.19mL

23.87mL

4.77mL

2.39mL
参考文献

[1]Peukert S, Hughes R, Nunez J, He G, Yan Z, Jain R, Llamas L, Luchansky S, Carlson A, Liang G, Kunjathoor V, Pietropaolo M, Shapiro J, Castellana A, Wu X, Bose A. Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists. ACS Med Chem Lett. 2014 Aug 4;5(10):1114-8

[2]Shimizu Y, Koyama R, Kawamoto T. Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation. Biochem Pharmacol. 2017 Sep 15;140:105-114