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L-006235

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Chemical Structure| 294623-49-7 同义名 : L-235
CAS号 : 294623-49-7
货号 : A753567
分子式 : C24H30N6O2S
纯度 : 99%+
分子量 : 466.599
MDL号 : MFCD18086856
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(64.3 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 L-006235, also known as L-235, is a potent, selective, reversible and orally active cathepsin K inhibitor with an IC50 of 5 nM in bone resorption assay.Compared to cathepsin B, cathepsin L and cathepsin S (Ki=1, 6 and 47 μM, respectively), the effects of L-006235 on cathepsin K (Ki=1, 6 and 47 μM) were significant. Compared with cathepsin B, chepsin L and cathepsin S (Ki = 1, 6 and 47 μM, respectively), L-006235 is more selective for cathepsin K (Ki = 0.2 nM), and L-006235 reduces collagen degradation and prevents bone loss[1][2].In a rabbit bone resorption assay, L-006235 inhibited bone resorption with an IC50 of 5 nM[1] .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.72mL

2.14mL

1.07mL

21.43mL

4.29mL

2.14mL
参考文献

[1]Palmer JT, et, al. Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J Med Chem. 2005 Dec 1;48(24):7520-34.

[2]Falgueyret JP, et, al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43.