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Submit ReviewL 006235 is a potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S. Displays reduced selectivity in cell-based assays possibly due to lysosomal accumulation. Reduces collagen breakdown and promotes bone deposition in vivo. Orally active and has intrinsic fluorescence.
L 006235 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 466.6 |
公式 | C24H30N6O2S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 294623-49-7 |
PubChem ID | 9912381 |
InChI Key | FIVYCSWOCXEWSE-UHFFFAOYSA-N |
Smiles | O=C(C2=CC=C(C3=CSC(N4CCN(C)CC4)=N3)C=C2)NC1(CCCCC1)C(NCC#N)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 46.66 | 100 |
以下数据基于产品分子量 466.6。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.14 mL | 10.72 mL | 21.43 mL |
5 mM | 0.43 mL | 2.14 mL | 4.29 mL |
10 mM | 0.21 mL | 1.07 mL | 2.14 mL |
50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
参考文献是支持产品生物活性的出版物。
Palmer et al (2005) Design and synthesis of tri-ring P3 benamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J.Med.Chem. 48 7520 PMID: 16302794
Falgueyret et al (2005) Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J.Med.Chem. 48 7535 PMID: 16302795
Desmarais et al (2008) Effects of cathepsin K inhibitors basicity on in vivo off-target activities. Mol.Pharmacol. 73 147 PMID: 17940194
If you know of a relevant reference for L 006235, please let us know.
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