Beta Amyloid
信号通路图
研究领域
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S2215 | DAPT (GSI-IX) | <1 mg/mL | 86 mg/mL | 50 mg/mL |
| S1575 | RO4929097 | <1 mg/mL | 93 mg/mL | 16 mg/mL |
| S2660 | MK-0752 | <1 mg/mL | 89 mg/mL | 45 mg/mL |
| S1262 | Avagacestat (BMS-708163) | <1 mg/mL | 104 mg/mL | <1 mg/mL |
| S1528 | LY2811376 | <1 mg/mL | 16 mg/mL | 64 mg/mL |
| s9087 | Tenuifolin | -1 mg/mL | 100 mg/mL | -1 mg/mL |
| S4261 | EUK 134 | 13 mg/mL | 83 mg/mL | <1 mg/mL |
| S4760 | (2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD) | 100 mg/mL | 100 mg/mL | 100 mg/mL |
| S5101 | Tabersonine hydrochloride | -1 mg/mL | 40 mg/mL | -1 mg/mL |
- Beta Amyloid抑制剂（9）
- 新Beta Amyloid产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2215 |
DAPT (GSI-IX)DAPT (GSI-IX)是一种新型γ-secretase抑制剂，抑制 Aβ产生，在HEK 293细胞中IC50为20 nM。 |
|
|
| S1575 |
RO4929097RO4929097是一种γ secretase抑制剂，无细胞试验中IC50为4 nM，抑制Aβ40和Notch的细胞加工，EC50分别为14 nM和5 nM。Phase 2。 |
(d,e) Effect of TUG1 overexpression on Nestin activity. Plasmid vectors expressing indicated genes were added to GSC-pE-Nes-222 treated with RO4929097. Phase-contrast and Nestin-EGFP images were shown in (d). Scale bars, 100 μm. (e) Intensity of Nestin-EGFP (left) and number of viable cells (right) compared with the DMSO control were quantified. Viable cells were assessed by trypan blue staining. *P<0.01, Kruskal–Wallis analysis. For all the experimental data, error bars indicate +s.d. (n=3).
|
|
| S2660 |
MK-0752MK-0752是一种适度有效的γ-secretase（γ-分泌酶）抑制剂，降低Aβ40产量，IC50为5 nM。Phase 1/2。 |
Jurkat cells were treated with (D) TRAIL (20 ng/ml), MK-0752 (50 µM) or a combination of the two for 48 h. Vehicle control for (D), 0.1% (v/v) dimethyl sulfoxide. Data shown are the mean ± standard error of the mean of ≥3 independent experiments. *P≤0.05, **P≤0.01. TRAIL, tumour necrosis factor-related apoptosis-inducing ligand.
|
|
| S1262 |
Avagacestat (BMS-708163)Avagacestat (BMS-708163)是口服生物有效的，选择性的γ-分泌酶抑制剂，作用于Aβ40和Aβ42时，IC50分别为0.3 nM和0.27 nM，比作用于Notch选择性高193倍。Phase 2。 |
A panel of GICs lines was treated with various concentrations of γ secretase inhibitors BMS-708163. Cells were treated with increasing concentrations of γ secretase inhibitors in triplicate wells for 72 hours, and cell viability was assessed by CellTiter-Blue assay as described in Materials and Methods. The results shown are of a single experiment with three independent replicates cell viability was measured by CellTiter-Blue assay. The graph depicts cell viability at 72 hours. Cell viability in the vehicle control was considered as to be 100%. |
|
| S1528 |
LY2811376LY2811376是第一个口服有效的，非肽类β-secretase(BACE1)抑制剂，IC50为239 nM-249 nM，可以减少Aβ分泌，EC50为300 nM，作用于BACE1比作用于BACE2选择性高10倍，比作用于其他天冬氨酸蛋白酶（包括Cathepsin D，胃蛋白酶和肾素）抑制效果高50倍以上。Phase 1。 |
|
|
| s9087New |
TenuifolinTenuifolin, a secondary saponin isolated from hydrolysates of polygalasaponins, inhibits beta-amyloid synthesis in vitro and has nootropic activity in vivo via acetylcholine esterase inhibition and increases norepinephrine and dopamine production. |
||
| S4261 |
EUK 134EUK 134是一种合成的超氧化物歧化酶（SOD）/过氧化氢酶类似物，具有强效的抗氧化活性，且抑制β-amyloid（β-淀粉样蛋白）和相关的淀粉样纤维形成。 |
||
| S4760 |
(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)HP-β-cyclodextrin (HP-β-CD), a well-known sugar used in drug delivery, genetic vector, environmental protection and treatment of Niemann-Pick disease type C1 (NPC1), is an inhibitor of amyloid-β aggregation. |
||
| S5101 |
Tabersonine hydrochlorideTabersonine, an ingredient extracted from the bean of Voacanga africana, is a potent inhibitor against Aβ(1−42) aggregation and toxicity. |
-LY2811376-J-Biol-Chem-20150727.gif)
-J-Biol-Chem-20150727.gif)
