2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. Cathepsin K-IN-9

Cathepsin K-IN-9 是一种选择性、强效且具有口服活性的 Cathepsin K 抑制剂，其 IC50 为 6.2 nM。Cathepsin K-IN-9 对组织蛋白酶 B、L 和 S 的 IC50 均大于 10000 nM，表现出超过 1600 倍的选择性。Cathepsin K-IN-9 具有优异的安全性和代谢稳定性，可用于骨质疏松症的研究。

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Cathepsin K-IN-9

Cathepsin K-IN-9 Chemical Structure

CAS No. : 2361420-28-0

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Cathepsin K-IN-9 相关抗体

Top Publications Citing Use of Products

查看 Cathepsin 亚型特异性产品:

查看所有亚型
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cathepsin K-IN-9 is a selective, potent and orally active Cathepsin K inhibitor with an IC50 of 6.2 nM. Cathepsin K-IN-9 has IC50 > 10000 nM for cathepsin B, L, and S, showing over 1600-fold selectivity. Cathepsin K-IN-9 has excellent safety and metabolic stability.Cathepsin K-IN-9 can be used for the research of osteoporosis[1].

IC50 & Target[1]

cathepsin K

6.2 nM (IC50)

体外研究
(In Vitro)

Cathepsin K-IN-9 (Compound 9d)(0.001–10 μM；72 小时) 在 HEK293T 细胞中表现出低细胞毒性[1]。
Cathepsin K-IN-9 (10 μM, 120 分钟) 对人 5 种主要 CYP 同工酶 (1A2、2C9、2C19、2D6、3A4) 的抑制作用较弱，无明显代谢相互作用风险[1]。
Cathepsin K-IN-9 在高浓度下对 hERG 通道有潜在抑制 (IC50 = 447 nM)，但治疗浓度下无明显心脏毒性风险[1]。
Cathepsin K-IN-9 在人、狗、大鼠、小鼠肝微粒体中具有一定代谢稳定性，30 分钟后剩余量分别为 77.1%、84.3%、57.6%、69.1%[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cathepsin K-IN-9 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T cells
Concentration: 0.001, 0.004, 0.01, 0.01, 0.1, 0.3, 1.1, 3.3 and 10 μM
Incubation Time: 72 h
Result: Maintained cell vitality at over 70%.
分子量

575.75

Formula

C35H41N7O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Cathepsin K-IN-9 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cathepsin K-IN-92361420-28-0CathepsinOsteoporosisCathepsin KCYP1A2CYP2C9CYP2C19CYP2D6CYP3A4hERGInhibitorinhibitorinhibit

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