PD-146176
| 中文名称 | PD-146176 |
|---|---|
| 中文同义词 | 6,11-二氢硫代色烯[4,3-B]吲哚;6,11-二氢硫代苯并吡喃并[4,3-B]吲哚;化合物PD146176;PD 146176,15-脂氧合酶抑制剂;化合物PD146176,10 MM DMSO 溶液 |
| 英文名称 | PD 146176 |
| 英文同义词 | 6,11-dihydrothiochromeno[4,3-b]indole;[1]Benzothiopyrano[4,3-b]indole, 6,11-dihydro-;PD146176 (NSC168807);NSC168807;inhibit,tau,brain,triple,NSC-168807,PD146176,Autophagy,pathology,amyloidosis,transgenic,reticulocyte,impairment,cognitive,mice,NSC 168807,Inhibitor,cells,PD 146176,IC21,PD-146176,rabbit,Ferroptosis;PD 146176;PD146176, 10 mM in DMSO |
| CAS号 | 4079-26-9 |
| 分子式 | C15H11NS |
| 分子量 | 237.32 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 4079-26-9.mol |
| 结构式 |  |
PD-146176 性质
| 熔点 | 160 °C |
|---|---|
| 沸点 | 485.4±24.0 °C(Predicted) |
| 密度 | 1.333±0.06 g/cm3(Predicted) |
| 储存条件 | Store at +4°C |
| 溶解度 | DMSO：16 mg/mL，可溶 |
| 形态 | 固体 |
| 酸度系数(pKa) | 16.17±0.20(Predicted) |
| 颜色 | 奶油色 |
| InChI | 1S/C15H11NS/c1-3-7-13-10(5-1)12-9-17-14-8-4-2-6-11(14)15(12)16-13/h1-8,16H,9H2 |
| InChIKey | ZGOOPZVQMLHPFM-UHFFFAOYSA-N |
| SMILES | C1Sc2ccccc2-c3[nH]c4ccccc4c13 |
PD146176 (NSC168807) 是一种有效的 15-lipoxygenase (15-LO) 的抑制剂，对rabbit reticulocyte 15-LO的Ki值为197 nM。
| Target | Value |
|
rabbit reticulocyte 15-LO
(Cell-free assay) | 197 nM(Ki) |
In intact IC21 cells transfected with human 15-LO, PD146176 inhibits 13-HODE production with an IC 50 of 0.81 μM.
PD146176 (80 mg/kg; Chowing; 12 weeks) reverses cognitive impairment, brain amyloidosis, and Tau pathology by stimulating autophagy in aged triple transgenic mice.
| Animal Model: | Triple transgenic (3xTg) mice |
| Dosage: | 80 mg/kg |
| Administration: | Chowing; 12 weeks |
| Result: | Significantly lower amyloid beta levels and deposition, less tau neuropathology, increased synaptic integrity, and autophagy activation. |
安全信息
| 安全说明 | 22-24/25 |
|---|---|
| WGK Germany | 3 |
| 存储类别 | 11 - 可燃固体 |