TC-G-1008
产品说明书
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同义名 : | GPR39-C3 |
| CAS号 : | 1621175-65-2 | |
| 货号 : | A724127 | |
| 分子式 : | C18H19ClN6O2S | |
| 纯度 : | 98%+ | |
| 分子量 : | 418.9 | |
| MDL号 : | MFCD30182283 | |
| 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 |
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| 溶解度 : | - | |
| 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 | |
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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 |
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