- TC-G 1008
货号： abs812279
| 货号-规格 | 货期 | 价格 | 数量 |
| abs812279-5mg | 1-2周 | ￥1147.00 | - + |
| abs812279-10mg | 1-2周 | ￥1764.00 | - + |
大包装询价| 产品描述 | ||
| 描述 | TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively). | |
| 纯度 | 98% | |
| 储存/保存方法 | store at -20℃ for one year（Powder）；
in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. | |
| 基本信息 | ||
| 别名 | TC-G 1008 | |
| 外观 | Solid powder | |
| 可溶性/溶解性 | DMSO : ≥100 mg/mL | |
| 生物活性 | ||
| 靶点 | GHSR | |
| In vitro(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. | |
| In vivo(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. | |
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Certificate of Analysis(COA)
