4079-26-9
中文名稱
PD-146176
英文名稱
PD 146176
CAS
4079-26-9
分子式
C15H11NS
分子量
237.32
MOL 文件
4079-26-9.mol
更新日期
2024/07/18 22:51:47
4079-26-9 結(jié)構(gòu)式
基本信息
中文別名
化合物PD1461766,11-二氫硫代色烯[4,3-B]吲哚
6,11-二氫硫代苯并吡喃并[4,3-B]吲哚
英文別名
6,11-dihydrothiochromeno[4,3-b]indole[1]Benzothiopyrano[4,3-b]indole, 6,11-dihydro-
物理化學(xué)性質(zhì)
熔點(diǎn)160 °C
沸點(diǎn)485.4±24.0 °C(Predicted)
密度1.333±0.06 g/cm3(Predicted)
儲(chǔ)存條件Store at +4°C
溶解度DMSO: 16 mg/mL, soluble
溶解度DMSO：16 mg/mL，可溶
酸度系數(shù)(pKa)16.17±0.20(Predicted)
形態(tài)solid
顏色cream-colored
常見問(wèn)題列表
生物活性
PD146176 (NSC168807) 是一種有效的 15-lipoxygenase (15-LO) 的抑制劑，對(duì)rabbit reticulocyte 15-LO的Ki值為197 nM。靶點(diǎn)
| Target | Value |
|
rabbit reticulocyte 15-LO
(Cell-free assay) | 197 nM(Ki) |
體外研究
In intact IC21 cells transfected with human 15-LO, PD146176 inhibits 13-HODE production with an IC 50 of 0.81 μM.
體內(nèi)研究
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. |