Odanacatib (MK-0822)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Odanacatib（MK-0822）是组织蛋白酶K的强效的、口服的选择性抑制剂，IC50值为0.2 nM [1]。
组织蛋白酶K主要表达在破骨细胞中，降解骨的胶原基质成分，在介导骨吸收中发挥中心作用。Odanacatib作为组织蛋白酶K的抑制剂，可用于治疗骨质疏松症。临床前证据和临床IIB期剂量范围试验提供的临床数据表明，odanacatib可以减少骨吸收，但在一定程度保留了女性绝经后的骨形成。目前，Odanacatib正在进行III期临床试验分析，对大于16000例绝经后骨质疏松症患者进行降低骨折风险的评估[2]。
参考文献：
[1] S. Aubrey Stoch, Stefan Zajic, Julie A. Stone, Deborah L. Miller, Lucas van Bortel, Kenneth C. Lasseter, Barnali Pramanik, Caroline Cilissen, Qi Liu, Lida Liu, Boyd B. Scott, Deborah Panebianco, Yu Ding, Keith Gottesdiener & John A. Wagner. Odanacatib, a selective cathepsin K inhibitor to treat osteoporosis: safety, tolerability, pharmacokinetics and pharmacodynamics –results from single oral dose studies in healthy volunteers. British Journal of Clinical Pharmacology. 2012, 75, (5): 1240-1254.
[2] Matt S. Anderson, Isaias Noel Gendrano, Chengcheng Liu, Steven Jeffers, Chantal Mahon, Anish Mehta, Kate Mostoller, Stefan Zajic, Denise Morris, Jessie Lee, and S. Aubrey Stoch. Odanacatib, a selective Cathepsin K inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. Endocrine Research. 2014, 99(2):552–560.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 525.56 |
| Cas No. | 603139-19-1 |
| Formula | C25H27F4N3O3S |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥17.7 mg/mL in DMSO |
| Chemical Name | (2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C)(CC(C(=O)NC1(CC1)C#N)NC(C2=CC=C(C=C2)C3=CC=C(C=C3)S(=O)(=O)C)C(F)(F)F)F |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| MK-0822是半胱氨酸蛋白酶组织蛋白酶K的强效选择性抑制剂，IC50值为0.2 nM，对组织蛋白酶B （cathepsin B）、L和S的IC50分别为1034 nM、2995 nM和60 nM。 ) | ||||||
| 靶点 | cathepsin K | |||||
| IC50 | 0.2nM | |||||
质量控制和MSDS
- 批次:
化学结构
