Home > Cysteine Protease & > Odanacatib

Odanacatib

奥当卡替,MK-0822,MK 0822,MK0822

Odanacatib (MK-0822)是一种有效的，选择性的，cathepsin K(人/兔)中性抑制剂，IC50为0.2 nM/1 nM，对脱靶的cathepsin B， L， S具有高度选择性。

目录号
EY0624
EY0624
EY0624
纯度
99.67%
99.67%
99.67%
规格
2 mg
5 mg
10 mg
原价
890
1400
2500
售价
890
1400
2500
库存
现货
现货
现货
订购
订购
订购
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  • 生物活性

    Odanacatib (MK 0822) is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

  • 动物实验

    ≤9 µM/day口服处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Gauthier JY, et al. Bioorg Med Chem Lett. 2008, 18(3), 923-928.
    [2] Jacques Yves Gauthier, Nathalie ChauretThe discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K Bioorganic & Medicinal Chemistry Letters Volume 18, Issue 3, 1 February 2008, Pages 923-928
    [3] Sun L, Forni S, Schwartz MS, Breidinger S, Woolf EJ.Quantitative determination of odanacatib in human plasma using liquid-liquid extraction followed by liquid chromatography-tandem mass spectrometry analysis.J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Feb 15;885-886:15-23. Epub 2011 Dec 13.

    分子式
    C25H27F4N3O3S    		 分子量
    525.56    		 CAS号
    603139-19-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    100 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT01803607 Osteoporosis Drug: odanacatib|Other: placebo to odanacatib Merck Sharp & Dohme Corp. Phase 3 2013-03-01 2014-12-30
    NCT00769418 Osteoporosis Drug: odanacatib|Drug: Comparator: Placebo Merck Sharp & Dohme Corp. Phase 1 2004-09-01 2015-08-18
    NCT01068262 Osteoporosis Drug: Odanacatib|Drug: Comparator: Placebo Merck Sharp & Dohme Corp. Phase 1 2009-12-01 2015-04-01
    NCT01512693 Hepatic Insufficiency Drug: Single Dose MK-0822 Merck Sharp & Dohme Corp. Phase 1 2012-02-01 2015-07-17
    NCT01512667 Renal Insufficiency Drug: MK-0822 Merck Sharp & Dohme Corp. Phase 1 2012-01-01 2016-02-03
    NCT00863525 Osteoporosis Drug: odanacatib|Drug: Comparator: Placebo Merck Sharp & Dohme Corp. Phase 1 2004-11-01 2015-08-18
    NCT00691899 Prostate Cancer Drug: odanacatib|Drug: placebo (unspecified) Merck Sharp & Dohme Corp. Phase 3 2008-09-01 2016-08-11
    NCT01120600 Osteoporosis Drug: Odanacatib|Drug: Placebo for Odanacatib Merck Sharp & Dohme Corp. Phase 3 2010-06-01 2015-10-14
    NCT01630616 Osteoporosis Drug: Odanacatib|Drug: Placebo Merck Sharp & Dohme Corp. Phase 1 2013-03-01 2016-09-26
    NCT00692458 Breast Cancer Drug: Comparator: odanacatib|Drug: Comparator: placebo Merck Sharp & Dohme Corp. Phase 3 2008-09-01 2016-08-11
    NCT00529373 Postmenopausal Osteoporosis Drug: Odanacatib|Drug: Placebo for Odanacatib|Dietary Supplement: Vitamin D3 Merck Sharp & Dohme Corp. Phase 3 2007-09-01 2017-02-09
    NCT00620113 Osteoporosis Postmenopausal Drug: Odanacatib|Dietary Supplement: Vitamin D3|Dietary Supplement: Calcium carbonate|Drug: Placebo Merck Sharp & Dohme Corp. Phase 2 2007-12-01 2017-01-23
    NCT00770159 Osteoporosis Drug: odanacatib|Drug: Comparator: placebo to MK0822 Merck Sharp & Dohme Corp. Phase 1 2004-11-01 2016-02-04
    NCT01552122 Osteoporosis|Postmenopausal Osteoporosis Drug: Odanacatib|Drug: Alendronate|Other: Placebo (odanacatib)|Dietary Supplement: Cholecalciferol (Vitamin D3)|Dietary Supplement: Calcium carbonate|Other: Placebo (alendronate) Merck Sharp & Dohme Corp. Phase 3 2012-05-01 2015-08-26
    NCT00729183 Osteoporosis Drug: Odanacatib|Drug: Placebo Merck Sharp & Dohme Corp. Phase 3 2008-10-01 2015-12-11
    NCT00885170 Osteoporosis Drug: odanacatib|Drug: Comparator: Placebo|Dietary Supplement: Vitamin D3|Dietary Supplement: Calcium Merck Sharp & Dohme Corp. Phase 2 2009-04-01 2015-02-12
    NCT00863590 Osteoporosis Drug: odanacatib|Drug: Comparator: odanacatib (Panel B)|Drug: Comparator: odanacatib (Panel C)|Drug: Comparator: odanacatib (Panel D) Merck Sharp & Dohme Corp. Phase 1 2004-06-01 2015-08-18
    NCT00399802 Breast Cancer|Metastatic Bone Disease Drug: Odanacatib|Drug: Comparator: zoledronic acid|Drug: Comparator: Placebo (unspecified)|Drug: Comparator: Placebo (unspecified) Merck Sharp & Dohme Corp. Phase 2 2006-11-01 2015-02-12
    NCT00112437 Osteoporosis Drug: MK0822|Drug: MK0822|Drug: MK0822|Drug: MK0822|Dietary Supplement: Vitamin D3|Dietary Supplement: Calcium Carbonate|Drug: Placebo Merck Sharp & Dohme Corp. Phase 2 2005-06-01 2016-03-03
    NCT00397683 Osteoarthritis Drug: MK0822 Merck Sharp & Dohme Corp. Phase 2 2006-10-01 2015-10-30
    NCT00242476 Vitamin D Deficiency Drug: MK0822A Merck Sharp & Dohme Corp. Phase 2 2005-09-01 2015-05-13

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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