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SID 26681509

现货
Catalog No.
A4424
人组织蛋白酶L抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 4,816.00
Ship with 10-15 days

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Background

IC50: 56 nM

SID 26681509 is a potent and reversible human cathepsin L inhibitor.

The cathepsins have been found to comprise a family of lysosomal protease enzymes whose primary functions, such as protein degradation, play a keyl role in normal cellular homeostasis. Overexpression of cathepsin L and/or abnormal activity has been implicated in a number of disease states.

In vitro: SID 26681509 was found to inhibit human cathepsin L with an IC50 of 56 nM. After preincubation with enzyme for 1, 2, and 4 h before substrate addition, SID 26681509 showed increasing potency, with IC50 values falling to 7.5, 4.2, and 1.0 nM, respectively, indicating a slow onset of inhibition. SID 26681509 was also observed to be nontoxic to human aortic endothelial cells up to 100 μM. SID 26681509 was active in an in vitro propagation assay against P. falciparum with an IC50 of 15.4 μM. Additionally, the thiocarbazate inhibitor was toxic toward L. major promastigotes with an IC50 of 12.5 μM [1].

In vivo: SID 26681509 showed a lack of toxicity to zebrafish in a live organism assay at 100 μM [1].

Clinical trial: N/A

Reference:
[1] Shah PP,Myers MC,Beavers MP,Purvis JE,Jing H,Grieser HJ,Sharlow ER,Napper AD,Huryn DM,Cooperman BS,Smith AB 3rd,Diamond SL.  Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L. Mol Pharmacol.2008 Jul;74(1):34-41.

Chemical Properties

Physical AppearanceWhite solid
StorageStore at -20°C
M.Wt539.65
Cas No.958772-66-2
FormulaC27H33N5O5S
Solubility<26.98mg/ml in DMSO; <5.4mg/ml in ethanol
Chemical Name(S)-S-(2-((2-ethylphenyl)amino)-2-oxoethyl) 2-(2-((tert-butoxycarbonyl)amino)-3-(1H-indol-3-yl)propanoyl)hydrazinecarbothioate
SDFDownload SDF
Canonical SMILESO=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[C@H](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人类主动脉内皮细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

100 μM,37°C,24h

应用

SID 26681509(100 μM)对人主动脉内皮细胞无毒性。在针对恶性疟原虫的体外繁殖实验中,SID 26681509具有活性,IC50为15.4 ± 0.6 μM。SID 26681509对L.主要前鞭毛体具有毒性,IC50为12.5 ± 0.6 μM。

动物实验 [1]:

动物模型

斑马鱼

给药剂量

100 μM

应用

在活体生物实验中,SID 26681509 (100 μM)对斑马鱼没有毒性。

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Shah P P, Myers M C, Beavers M P, et al. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L[J]. Molecular pharmacology, 2008, 74(1): 34-41.

生物活性

Potent and reversible human cathepsin L inhibitor (IC50 = 56 nM).
Targets cathepsin L          
IC50 56nM          

质量控制

质量控制和MSDS

批次:

化学结构

SID 26681509