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L-685458 (Synonyms: L-685,458) 纯度: 99.33%
L-685458 是一种有效的过渡状态模拟(TSA) γ-分泌酶 (γ-secretase) 抑制剂 (GSI)。L-685458 抑制淀粉样 β-蛋白前体 γ-分泌酶活性,IC50 为 17 nM,选择性高于其他检测的天冬氨酸蛋白酶 50-100 倍。L-685458 抑制 γ-分泌酶介导的 APP-C99 和 Notch-100 的裂解,IC50 分别为 301.3 nM 和 351.3 nM。L-685458 可用于阿尔茨海默病 (AD) 和癌症的研究。
L-685458 Chemical Structure
CAS No. : 292632-98-5
规格 | 价格 | 是否有货 | 数量 |
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10 mM * 1 mL in DMSO | ¥7253 | In-stock | |
1 mg | ¥1400 | In-stock | |
5 mg | ¥4900 | In-stock | |
10 mg | ¥8800 | In-stock | |
50 mg | 询价 | ||
100 mg | 询价 |
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L-685458 相关产品
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生物活性 |
L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers[1][2]. |
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体外研究 (In Vitro) |
L-685458 reduces both Aβ(40) and Aβ(42) peptide formation in 3 different cells. It against Neuro2A h AβPP695, CHO h AβPP695, and SHSY5 spβA4CTF reduction of Aβ(40) with IC50 values of 402 nM, 113 nM and 48 nM, respectively. And the IC50 values are 775 nM, 248 nM, 67 nM, respectively[1].L-685458 (5-40 μM; 24 hours) leads to a dramatic downregulation of Hes-1 in 786-O cells[3].L-685458 has inhibitory effects in hepatoma cell lines, it against Huh7, HepG2, HLE and SKHep1 cells with IC50 of 12.91 μM, 12.69 μM, 21.76 μM and 12.18 μM, respectively[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
L-685458 (percutaneous administration; 5 mg/kg; 2 weeks) has antitumor effects in mouse hepatoma models. L-685458 inhibits EpCAM production except in necrotic areas. And HES1 staining is also diminished in the nucleus[4]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
672.85 |
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Formula |
C39H52N4O6 |
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CAS 号 |
292632-98-5 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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溶解性数据 |
In Vitro:
DMSO : 83.3 mg/mL (123.80 mM; Need ultrasonic and warming) 配制储备液
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
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参考文献 |
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