| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S83712-1mg买3赠1 |
98.30% | ￥240.00 |
10 | - | - | - | - |
|
S83712-2mg买3赠1 |
98.30% | ￥380.00 |
9 | - | - | - | - |
|
S83712-5mg买3赠1 |
98.30% | ￥570.00 |
6 | - | - | - | - |
|
S83712-10mg买3赠1 |
98.30% | ￥700.00 |
3 | - | - | - | - |
|
S83712-25mg买3赠1 |
98.30% | ￥1290.00 |
2 | - | - | - | - |
|
S83712-50mg买3赠1 |
≥98% | ￥2280.00 |
货期：2-3天 | - | - | - | - |
|
S83712-100mg买3赠1 |
≥98% | ￥3800.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | TC-G-1008 (GPR39-C3) is a potent and orally available GPR39 agonist with EC50 values of 0.4 and 0.8 nM for rat and human receptors respectively. | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | IC50: 0.4 nM (GPR39), 0.8 nM (GPR39);GHSR | ||||||||||||||||||||
| 体外研究： | TC-G-1008 shows selectivity over a panel of kinases (IC50s>10 μM) and does not exhibit relevant binding affinity for the related ghrelin and neurotensin-1 receptors (IC50s>30 μM). In HEK293-GPR39 cells, GPR39-C3, which is a positive allosteric modulator, activates cAMP production (downstream of Gs), IP1 accumulation (downstream of Gq), SRF-RE-dependent transcription (downstream of G12/13), and β-arrestin recruitment. GPR39-C3 induces dose- and time-dependent loss of response in cAMP production by second challenge of the compound | ||||||||||||||||||||
| 体内研究： | Rat and mouse plasma protein binding for TC-G-1008 is measured as 99.3% and 99.1%, respectively. TC-G-1008 is orally bioavailable in mice and robustly induces acute GLP-1 levels. Upon single oral doses of 10, 30, and 100 mg/kg of aqueous suspensions in 0.5% methylcellulose/0.1% Tween 80, TC-G-1008 achieves, between 1 and 1.5 h, maximal exposures of 1.4, 6.1, and 25.3 μM, respectively | ||||||||||||||||||||
| 参考文献： | 1. Peukert S, et al. 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, et al. Rho kinase-dependent desensitization of GPR39; a unique mechanism of GPCR downregulation. Biochem Pharmacol. 2017 Sep 15;140:105-114. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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