Odanacatib (MK-0822)
(Synonyms: 奥当卡替; MK-0822) 目录号 : GC16388
A potent, selective, and neutral inhibitor of cathepsin K
Cas No.:603139-19-1
Sample solution is provided at 25 µL, 10mM.
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Odanacatib (MK-0822) is a potent, orally active and selective inhibitor of Cathepsin K with IC50 value of 0.20 nM [1],
Cathepsin K is expressed predominantly in osteoclasts and degrades the collagen matrix componentsofbone. It plays a central role in mediating bone resorption. And the inhibitor of cathepsin K, Odanacatib, is in development for the treatment of osteoporosis. Based on preclinical evidence and available clinical data from dose-ranging phase IIB trials, odanacatib appears to reduce bone resorptionwhile somewhat preserving bone formation in postmenopausal
Women. Currently, Odanacatib is undergoing evaluation for fracture risk reduction in a phase III trial with ＞16000 patients with postmenopausal osteoporosis [2].
References:
[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.
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Cell experiment: |
To assess cell survival, differentiated osteoclast (OC) at appr 7×104 cells/cm2 are re-seeded on bovine bone slices with or without 100 nM Odanacatib (ODN). Bone slices are fixed on days 2, 4, 6, and 12 with no media changes. Samples are stained for TRAP activity, and OC number. |
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Animal experiment: |
Sixteen, 8-month-old, female Sprague-Dawley (SD) rats (weight, 385 ± 55 g) are given water and soft diet food ad libitum in a temperature-controlled environment with regular 12-h cycles of light and dark. The rats are randomised into 4 groups, with 4 rats in each group: sham group, OVX + Veh group, OVX + ODN-l group and OVX + ODN-h group. Following implant insertion, Odanacatib (ODN, 5 mg/mL) is administered to the OVX + ODN-l and OVX + ODN-h groups at concentrations of 1 mL/kg and 6 mL/kg, respectively, by gavaging once a day for 8 weeks. The OVX + Veh group is gavaged with 0.5% sodium carboxymethyl cellulose at a concentration of 6 mL/kg over the same duration. After the gavage administration, the rats of each group are sacrificed by injecting sodium pentobarbital intravenously. The implants are harvested and fixed in 10% buffered formalin together with the surrounding bone. |
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References: [1]. Jacques Yves Gauthier, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. |
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| Cas No. | 603139-19-1 | SDF | |
| 别名 | 奥当卡替; MK-0822 | ||
| 化学名 | (2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide | ||
| 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 | ||
| 分子式 | C25H27F4N3O3S | 分子量 | 525.56 |
| 溶解度 | ≥ 17.7mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9027 mL | 9.5137 mL | 19.0273 mL |
| 5 mM | 0.3805 mL | 1.9027 mL | 3.8055 mL |
| 10 mM | 0.1903 mL | 0.9514 mL | 1.9027 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet