LY 303511,英文名:LY 303511,CAS:154447-38-8,化学式:C19H18N2O2,分子量:306.36,密度:1.237±0.06 g/cm3(Predicted),沸点:
154447-38-8
LY 303511(LY 303511)
CAS: 154447-38-8
化学式: C19H18N2O2
| 中文名 | LY 303511 |
| 英文名 | LY 303511 |
| 别名 | 化合物LY 303511 8-苯基-2-(1-哌嗪基)-4H-1-苯并吡喃-4-酮 |
| 英文别名 | LY303511 LY 303511 LY-303511(Nv-128) 8-Phenyl-2-(1-piperazinyl)-4H-1-benzopyran-4-one 2-(1-Piperazinyl)-8-phenyl-4H-1-benzopyran-4-one 4H-1-Benzopyran-4-one, 8-phenyl-2-(1-piperazinyl)- 8-Phenyl-2-(1-piperazinyl)-4H-1-benzopyran-4-one LY303511 |
| CAS | 154447-38-8 |
| 化学式 | C19H18N2O2 |
| 分子量 | 306.36 |
| 密度 | 1.237±0.06 g/cm3(Predicted) |
| 沸点 | 496.1±45.0 °C(Predicted) |
| 溶解度 | 10毫米DMSO |
| 酸度系数 | 9.20±0.10(Predicted) |
| 存储条件 | Store at +4°C |
| 外观 | 琥珀色固体 |
| 体外研究 | LY303511 is structurally identical to LY294002 except for a substitution of -O for -NH in the morpholine ring, and does not potently inhibit PI3K. Treatment of cells with LY303511 causes an increase in calcein spread similar to levels of LY294002. The ability of LY303511 to increase gap junctional intercellular communication (GJIC) does not occur concomitant with inhibition of phosphorylation of AKT as measured by immunoblotting. LY303511 enhances TRAIL sensitivity of SHEP-1 neuroblastoma cells via H 2 O 2 -MAPK activation and up-regulation of death receptors. SHEP-1 cells are exposed to varying concentrations of LY303511 (LY30), TRAIL, and a combination of the two (1 h preincubation with LY303511 followed by TRAIL for 4 hours). SHEP-1 cells are responsive to TRAIL (~10%, ~15%, and ~30% reduction in the surviving fraction at 25, 50, and 100 ng/mL, respectively); however, treatment with LY303511 (12.5, 25, or 50 μM) has no effect on cell viability. However, incubation of cells with LY303511 (25 μM) for 1 hour followed by 4 hours exposure to 50 ng/mL of TRAIL has a strong synergistic effect (~40% reduction in viable cells with LY303511+TRAIL versus ~15% with TRAIL alone). LY303511 is a negative control compound with respect to PI3K activity. In MIN6 insulinoma cells, Wortmannin (100 nM) has no effect on whole-cell outward K + currents, but LY294002 and LY303511 reversibly block currents in a dose-dependent manner (IC 50 =9.0±0.7 μM and 64.6±9.1 μM, respectively). Kv2.1 and Kv1.4 are highly expressed in beta-cells, and in Kv2.1-transfected tsA201 cells, 50 μM LY294002 and 100 μM LY303511 reversibly inhibit currents by 99% and 41%, respectively. LY303511 blocks currents with an IC 50 of 64.6±9.1 µM, with a maximal inhibition of ~90% at 500 µM (n≥5 cells at each concentration). |
| 体内研究 | Intraperitoneal administration of vehicle or LY303511 (10 mg/kg/day) is performed when tumors reach a volume of ~150 mm 3 , at which time 35 mice have developed a tumor. After 21 days, >15% of the mice require euthanasia because of excessive tumor growth, and these data are censored due to unreliable estimates of average tumor volume. The administration of LY303511, 10 mg/kg/day, is sufficient to inhibit PC-3 tumor growth in vivo. |
154447-38-8 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.264 ml | 16.321 ml | 32.642 ml |
| 5 mM | 0.653 ml | 3.264 ml | 6.528 ml |
| 10 mM | 0.326 ml | 1.632 ml | 3.264 ml |
| 5 mM | 0.065 ml | 0.326 ml | 0.653 ml |
154447-38-8 - 简介
LY 303511是一种化学物质，它是一种糖基转移酶抑制剂。它的化学名为（4R,5S,6S,7S,9R,10R,11R,12S,13E,15E,17E)-4,6,11-trihydroxy-10,12-dimethyl-2-oxo-13-[(2R,3R,4S,5S)-3,4,5-trihydroxy-6-methyloxan-2-yl]oxacyclohexadeca-13,15,17-triene-7-carbaldehyde。LY 303511主要用于研究和治疗糖尿病和肥胖症等疾病。它作为一种糖基转移酶抑制剂，可抑制葡萄糖生成的酶，进而减少葡萄糖的合成并降低血糖水平。它还具有抗炎和抗肿瘤的作用。
LY 303511的制法较为复杂，主要通过有机合成方法得到。一般来说，它是通过一系列化学反应，包括羟基保护、环化反应和羟基去保护等步骤进行合成的。
LY 303511属于实验室级别的化学品，必须遵守实验室安全操作规程。
在操作过程中应避免直接与皮肤和眼睛接触，并注意避免吸入其粉尘或溶液。
使用前应仔细阅读并遵循相关的安全数据表和操作说明。
应妥善保存LY 303511，远离火源和易燃物质。
如果出现异常情况（如吸入、皮肤接触、误食等），应立即求医并提供医生相关信息。
最后更新：2024-04-09 20:52:54
