LY2608204 (LY2608204) 是葡萄糖激酶 (GK) 的激活剂，EC50 为 42 nM。
| Cas No. | 1234703-40-2 |
| 别名 | (1R,2S)-2-环己基-1-[4-(环丙基磺酰基)苯基]-N-[5-[[2-(1-吡咯烷基)乙基]硫代]-2-噻唑基]环丙烷甲酰胺,LY2608204 |
| 化学名 | (1R,2S)-2-cyclohexyl-1-(4-cyclopropylsulfonylphenyl)-N-[5-(2-pyrrolidin-1-ylethylsulfanyl)-1,3-thiazol-2-yl]cyclopropane-1-carboxamide |
| Canonical SMILES | C1CCC(CC1)C2CC2(C3=CC=C(C=C3)S(=O)(=O)C4CC4)C(=O)NC5=NC=C(S5)SCCN6CCCC6 |
| 分子式 | C28H37N3O3S3 |
| 分子量 | 559.81 |
| 溶解度 | ≥ 28.35mg/mL in DMSO |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | LY2608204 is a activator of glucokinase (GK) with EC50 of 42 nM.IC 50 value: 42 nM (EC50)Target: glucokinasein vitro: LY2608204 activates glucokinase (GK) with EC50 of 42 nM at 10 mM glucose with a concentration dependent manner at lower glucose concentrations. LY2608204 also stimulates glucose metabolism in rat insulinoma INS1-E cells with EC50 of 579 nM.in vivo: LY2608204 decreases plasma glucose in a dose-dependent manner at both fasted and postprandial glucose levels. A maximal lowering of glucose AUC versus the untreated control group is observed with the high dose (30 mg/kg) and represents a 42% decrease. Interpolation of the data show that a 20% glucose AUC decrease occurs at an average LY2608204 concentration of 99 ng/mL (179 nM) in plasma, corresponding to a 6.9 mg/kg LY2608204 dose. The in vivo blood brain barrier permeability of LY2608204 results in a mean brain/plasma ratio of 0.17 five minutes post-dose with a mean total brain level of 0.539 nmol/g.Clinical trail: |
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