L-873724
目录号: PL15156 纯度: ≥98%
CAS No. :603139-12-4
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中文名称
L-873724
英文名称
L-873724
英文别名
MK-0822;29250PP3ON;(2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide;VYFDSJLOCIGIKP-SFTDATJTSA-N;L873724;GTPL7860;BDBM19489;Pentanamide, N-(cyanomethyl)-4-methyl-2-(((1S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)(1,1'-biphenyl)-4-yl)ethyl)amino)-, (2S)-;Q27078443;(2S)-N-(cyanomethyl)-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-;L-873724
Cas No.
603139-12-4
分子式
C23H26F3N3O3S
分子量
481.53
包装储存
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
产品详情
L-873724 是一种有效、可口服、选择性、可逆的非碱性 cathepsin K 抑制剂,对 cathepsin K,cathepsin S,cathepsin L,cathepsin B 的 IC50 值分别为 0.2,178,264 和 5239 nM。L-873724 抑制兔子 cathepsin K 的活性,IC50 值为 0.5 nM,同时可抑制骨再吸收。
生物活性
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC 50 s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC 50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.
性状
Solid
IC50 & Target[1][2]
IC50: 0.2 nM (Cathepsin K), 178 nM (Cathepsin S), 264 nM (Cathepsin B), 5239 nM (Cathepsin B), 0.5 nM (Rabbit cathepsin K)
体外研究(In Vitro)
L-873724 (Compound 22) is a potent and selective non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also shows IC50s of 95, 1221 and 4807 nM for Ramos cathepsin S, Hep G2 cathepsin L, Hep G2 cathepsin B. L-873724 exhibits an IC50 of 0.5 nM for rabbit cathepsin K. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
L-873724 is orally bioavailable, non-lysosomotropic, and efficacious in the rhesus monkey bone resorption model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
参考文献
[1]. Li CS, et al. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9.
[2]. Zhuo Y, et al. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone. 2014 Oct;67:269-80.
溶解度数据
In Vitro: DMSO : 100 mg/mL (207.67 mM; Need ultrasonic)配制储备液
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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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