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CAS No.: 1621175-65-2

TC-G-1008 Catalog No. CSN24454

Synonyms: GPR39-C3

TC-G 1008 is a selective GPR39 agonist with EC50 value of 0.8 nM.

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靶点选择性

生物活性

实验方案

技术信息

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].
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

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
- 2.3872 mL
- 11.9360 mL
- 23.8720 mL
- 5 mM
- 0.4774 mL
- 2.3872 mL
- 4.7744 mL
- 10 mM
- 0.2387 mL
- 1.1936 mL
- 2.3872 mL

技术信息

CAS号

1621175-65-2

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

C18H19ClN6O2S

运输

蓝冰

分子量

418.90

别名

GPR39-C3

溶解度

DMSO	170.0 mg/mL (405.8 mM)
Water	insoluble

动物实验配方

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TC-G-1008 Catalog No. CSN24454

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