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L-685,458

γ分泌酶抑制剂，L-685458是一种有效的淀粉样β蛋白前体γ分泌酶抑制剂, IC50为17 nM,比作用于其他天冬氨酰蛋白酶选择性高50-100倍。

目录号: PC15677 纯度: ≥98%

CAS No. :292632-98-5

商品编号	规格	价格	会员价	是否有货	数量
PC15677-1mg	1mg	¥1372.00	请登录
PC15677-5mg	5mg	¥4410.00	请登录

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中文名称

L-685,458

中文别名

(5S)-(叔丁氧羰基氨基)-6-苯基-(4R)-羟基-(2R)-苄基己酰)-L-亮氨酰-L-苯丙氨酰胺;gamma-分泌酶抑制剂 X

英文名称

L-685,458

英文别名

L-Phenylalaninamide,N-[(2R,4R,5S)-5-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-leucyl-;N-[(2R,4R,5S)-5-[[(1,1-Dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6- phenyl-2-(phenylmethyl)hexy;L-685 458;L-685,458,(5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide;L685458;L-Phenylalaninamide,N-[(2R,4R,5S)-5-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-ph...;L-Phenylalaninamide,N-[(2R,4R,5S)-5-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-l;N-[(2R,4R,5S)-5-[[(1,1-DiMethylethoxy)carbonyl]aMino]-4-hydroxy-1-oxo-6- phenyl-2-(phenylMethyl)hexyl]-L-leucyl-L-phenylalaninaMide;N-[(2R,4R,5S)-5-[[(1,1-Dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6- phenyl-2-(phenylmethyl)hexyl]-L-leucyl-L-phenylalaninamide;N-[(2R,4R,5S)-5-[[(1,1-Dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-leucyl-L-phenyl...;(5S)-(t-Butoxycarbonylamino)-6-phenyl-(4R)hydroxy-(2R)benzylhexanoyl)-L-leu-L-phe-amide;(5S)-(tert-ButoxycarbonylaMino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninaMide;CID 145707669;L-685458;L-Phenylalaninamide, N-[(2R,4R,5S)-5-[[(1,1-dimethylethoxy)carbonyl]amino]-4-hydroxy-1-oxo-6-phenyl-2-(phenylmethyl)hexyl]-L-leucyl-;tert-butyl ((2S,3R,5R)-6-(((S)-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-5-benzyl-3-hydroxy-6-oxo-1-phenylhexan-2-yl)carbamate;tert-butyl ((2S,3R,5R)-6-(((S)-1-(((S)-1-amino-1-oxo-3-phenylpropan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)amino)-5-benzyl-3-hydr;l-685,458

Cas No.

292632-98-5

分子式

C₃₉H₅₂N₄O₆

分子量

672.85

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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.

性状

Solid

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.
L-685458 (5-40 μM; 24 hours) leads to a dramatic downregulation of Hes-1 in 786-O cells.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD-SCID Mouse Hepatoma Model
Dosage:	5 mg/kg
Administration:	Percutaneous administration; 5 mg/kg; 2 weeks
Result:	Exhibited anti-tumor activities in vivo.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Shearman, M.S., Beher, D., Clarke, E.E., Lewis, H.D., Harrison, T., Hunt, P., [Information]

[2]. Guanghui Yang, et al. Structural basis of γ-secretase inhibition and modulation by small molecule drugs. Cell. 2021 Jan 21;184(2):521-533.e14. [Information]

[3]. Jonas Sj?lund, et al. Suppression of renal cell carcinoma growth by inhibition of Notch signaling 体外研究 and in vivo. J Clin Invest. 2008 Jan;118(1):217-28. [Information]

[4]. Kazunori Kawaguchi, et al. Jagged1 DNA Copy Number Variation Is Associated with Poor Outcome in Liver Cancer. Am J Pathol. 2016 Aug;186(8):2055-2067. [Information]

溶解度数据

体外研究:

DMSO : 83.3 mg/mL (123.80 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4862 mL	7.4311 mL	14.8622 mL
5 mM	0.2972 mL	1.4862 mL	2.9724 mL
10 mM	0.1486 mL	0.7431 mL	1.4862 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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