Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 /
抑制剂/激动剂
肿瘤
/
代谢酶
蛋白酶 肿瘤干细胞
/
组织蛋白酶
Cysteine Protease
/ Odanacatib

奥当卡替 /Odanacatib {[allProObj[0].p_purity_real_show]}

货号：A328069 同义名： 奥达卡替 / MK-0822 Ambeed 开学季，买赠积分，赢豪礼

Odanacatib 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.

Odanacatib 化学结构 CAS号：603139-19-1
Odanacatib 化学结构
CAS号：603139-19-1
Odanacatib 3D分子结构
CAS号：603139-19-1
Odanacatib 化学结构 CAS号：603139-19-1
Odanacatib 3D分子结构 CAS号：603139-19-1
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} 		{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 咨询 - +
购物车0 收藏 询单

Odanacatib 纯度/质量文件 产品仅供科研

货号：A328069 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• JACS Au, 2024. Ambeed. [ A148168 ]
• JMC, 2024. Ambeed. [ A187643 ]
• JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]
• Biomacromolecules, 2024. Ambeed. [ A110759 ]
• Biomacromolecules, 2024. Ambeed. [ A203543 ]
更多 >
产品名称 Cysteine Protease ↓ 其他靶点 纯度
Z-FA-FMK ✔ {[allProObj[0].p_purity_real_show]}
Leupeptin hemisulfate ✔ {[allProObj[0].p_purity_real_show]}
PMSF ✔ {[allProObj[0].p_purity_real_show]}
PD 151746 +

μ-Calpain, IC50: 260 nM

m-calpain, IC50: 5.33 μM

 		{[allProObj[0].p_purity_real_show]}
Odanacatib ++++

Cathepsin K (human), IC50: 0.2 nM

Cathepsin K (rabbit), IC50: 1 nM

 		{[allProObj[0].p_purity_real_show]}
E-64 +++

Cysteine protease, IC50: 9 nM

 		{[allProObj[0].p_purity_real_show]}
E 64c ✔ {[allProObj[0].p_purity_real_show]}
E-64d ✔ {[allProObj[0].p_purity_real_show]}
MG-101 ✔ {[allProObj[0].p_purity_real_show]}
Calpeptin ++

Calpain II (porcine kidney), ID50: 40 nM

Calpain I (porcine erythrocytes), ID50: 52 nM

 		{[allProObj[0].p_purity_real_show]}
Cathepsin inhibitor 1 +++

Cathepsin L2, pIC50: 5.5

Cathepsin L, pIC50: 7.9

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Odanacatib 生物活性

靶点

  • Cysteine Protease

    Cathepsin K (human), IC50:0.2 nM

    Cathepsin K (rabbit), IC50:1 nM
描述 Cathepsin K (Cat K) is a lysosomal cysteine protease that is responsible for osteoclastic bone resorption. Odanacatib is a selective and reversible inhibitor of both human and rabbit Cat K with IC50 values of 0.2 nM and 1.0 nM, respectively[1]. Odanacatib reduced the release of collagen type I C-telopeptide of (CTx) at a dose-dependent manner with IC50 of 9.4 ± 1.0 nM in human osteoclasts. When treated with more than 10 nM odanacatib for 5 days, osteoclasts showed smaller discontinuous trails of resorption puts compared to untreated cells. Odanacatib up to 100 nM suppressed the accumulation of resorption surfacein osteoclasts 5 days after the treatment. The efficacy of odanacatib in reducing resorption area per multinucleated TRAP+ cell was determined with an IC50 value of 6.5 ± 3.5 nM. In mature osteoclasts plated on bone surface, 4-day treatment of 100 nM odanacatib stimulated the retention of intracellular vesicles and the expressions of Cat K and TRAP. Also, cells treated with odanacatib at the same condition showed dramatically accumulated numbers of bone matrix-contining vesicles compared to untreated controls[2]. In a study of 7- to 8-week-old male wild-type BALB/cJ mice with bacterial infection, the bone resorption in the periapical lesion areas was significantly reduced in the group with odanacatib (3.606 mg/kg/week) at 42 days. The number of osteoclasts and the mRNA level of Cat K were decreased in the infected mice with odanacatib (3.606 mg/kg/week) compared to the ones without treatment[3].
作用机制 Odanacatib inhibits Cat K by directly binding with Cys25 side chain of Cat K with a covalent bond[4].

Odanacatib 动物研究

Dose Monkey: 6 mg/kg, 30 mg/kg[5] (p.o., q.d.) Rat: 5 mg/kg, 30 mg/kg[6] (p.o.)
Administration p.o.

Odanacatib 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00242476 Vitamin D Deficiency Phase 2 Completed - -
NCT00397683 Osteoarthritis Phase 2 Terminated - United States, California ... 展开 >> Call for Information Palm Desert, California, United States, 92260 Call for Information Pomona, California, United States, 91767 Call for Information Torrance, California, United States, 90505 Call for Information Upland, California, United States, 91786 United States, Florida Call for Information Coral Gables, Florida, United States, 33134 Call for Information Hialeah, Florida, United States, 33010 Call for Information South Miami, Florida, United States, 33143-0000 United States, New York Call for Information Rochester, New York, United States, 14168 Call for Information Rochester, New York, United States, 14609 Call for Information Rochester, New York, United States, 14618 United States, Pennsylvania Call for Information Norristown, Pennsylvania, United States, 19401 Call for Information Perkasie, Pennsylvania, United States, 18944 Chile Merck Sharp & Dohme (I.A.) Corp. Santiago, Chile, 6761641 Colombia Frosst Laboratories Inc. Bogota, Cundinamarca, Colombia Mexico Merck Sharp & Dohme De Mexico, S.A. De C.V. Mexico, D.f., Mexico, 1090 Poland MSD Polska Sp. z o.o. Dzial Medyczny Warszawa, Poland, 00-867 收起 <<
NCT00112437 Osteoporosis Phase 2 Completed - -

Odanacatib 参考文献

[1]Gauthier JY, Chauret N, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008;18(3):923-8.

[2]Leung P, Pickarski M, et al. The effects of the cathepsin K inhibitor odanacatib on osteoclastic bone resorption and vesicular trafficking. Bone. 2011 Oct;49(4):623-35.

[3]Hao L, Chen W, et al. A small molecule, odanacatib, inhibits inflammation and bone loss caused by endodontic disease. Infect Immun. 2015;83(4):1235-45.

[4]Lu J, Wang M, et al. Advances in the discovery of cathepsin K inhibitors on bone resorption. J Enzyme Inhib Med Chem. 2018;33(1):890-904.

Odanacatib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.51mL

1.90mL

0.95mL

19.03mL

3.81mL

1.90mL

Odanacatib 技术信息

CAS号603139-19-1
分子式C25H27F4N3O3S
分子量 525.559
别名 奥达卡替 ;MK-0822
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 25 mg/mL(47.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

4% DMSO+corn oil 5 mg/mL

Tags: Odanacatib | 603139-19-1 | MK-0822 | MK0822 | MK 0822 | Cathepsin K Inhibitor | Metabolic Enzyme/Protease | Cathepsin | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Odanacatib 纯度/质量文件 | Odanacatib 亚型比较 | Odanacatib 生物活性 | Odanacatib 动物研究 | Odanacatib 临床数据 | Odanacatib 参考文献 | Odanacatib 实验方案 | Odanacatib 技术信息

Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 Ambeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z