L 006235

Pricing Availability   Qty
说明: Potent cathepsin K inhibitor
化学名: N-[1-[[(Cyanomethyl)amino]carbonyl]cyclohexyl]-4-[2-(4-methyl-1-piperazinyl)-4-thiazolyl]benzamide
纯度: ≥98% (HPLC)
说明书
引用文献
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生物活性 for L 006235

L 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.

化合物库 for L 006235

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。

技术数据 for L 006235

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.

溶解性数据 for L 006235

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 46.66 100

制备储备液 for L 006235

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.

选择批次从而根据批次分子量重新计算:
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

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产品说明书 for L 006235

分析证书/产品说明书
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参考文献 for L 006235

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


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