Odanacatib | 奥达卡替 | MK-0822 | Cathepsin K Inhibitor

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

货号：A328069 同义名： 奥达卡替 / MK-0822

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 3D分子结构
CAS号：603139-19-1

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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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

Cysteine Protease 亚型比较

产品名称	Cysteine Protease ↓ ↑	纯度
Z-FA-FMK	✔	99%+
Leupeptin hemisulfate	✔	97%
PMSF	✔	95%
PD 151746	+ m-calpain, IC50: 5.33 μM μ-Calpain, IC50: 260 nM	98%
Odanacatib	++++ Cathepsin K (rabbit), IC50: 1 nM Cathepsin K (human), IC50: 0.2 nM	99%+
E-64	+++ Cysteine protease, IC50: 9 nM	99%+
E 64c	✔	95%
E-64d	✔	99%+
MG-101	✔	98%+
Calpeptin	++ Calpain I (porcine erythrocytes), ID50: 52 nM Calpain II (porcine kidney), ID50: 40 nM	98%+
Cathepsin inhibitor 1	+++ Cathepsin L2, pIC50: 5.5 Cathepsin L, pIC50: 7.9	98%
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 (rabbit), IC50:1 nM Cathepsin K (human), IC50:0.2 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

液体 -20°C:3-6个月-80°C:12个月

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

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

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	-	-
NCT00863590	Osteoporosis	Phase 1	Completed	-	-
NCT00885170	Osteoporosis	Phase 2	Completed	-	-
NCT00770159	Osteoporosis	Phase 1	Completed	-	-
NCT00885170	-		Completed	-	-
NCT00399802	Breast Cancer ... 展开 >> Metastatic Bone Disease 收起 <<	Phase 2	Completed	-	-
NCT00399802	-		Completed	-	-
NCT00112437	-		Completed	-	-
NCT01552122	Osteoporosis ... 展开 >>Postmenopausal Osteoporosis 收起 <<	Phase 3	Withdrawn	February 2015	-
NCT00620113	Osteoporosis Postmenopausal	Phase 2	Completed	-	-
NCT00729183	Osteoporosis	Phase 3	Completed	-	-
NCT00729183	-		Completed	-	-
NCT00692458	Breast Cancer	Phase 3	Withdrawn(Withdrawn for admini... 展开 >>strative reasons) 收起 <<	September 2008	-
NCT01120600	Osteoporosis	Phase 3	Completed	-	-
NCT00529373	Postmenopausal Osteoporosis	Phase 3	Completed	-	-
NCT00863525	Osteoporosis	Phase 1	Completed	-	-
NCT00691899	Prostate Cancer	Phase 3	Withdrawn(Withdrawn for admini... 展开 >>strative reasons) 收起 <<	September 2008	-
NCT00769418	Osteoporosis	Phase 1	Completed	-	-
NCT01630616	-		Terminated	-	-
NCT00620113	-		Completed	-	-
NCT01068262	Osteoporosis	Phase 1	Completed	-	-
NCT01630616	Osteoporosis	Phase 1	Terminated	-	-
NCT01512693	-		Completed	-	-
NCT01512693	Hepatic Insufficiency	Phase 1	Completed	-	-
NCT01068262	-		Completed	-	-
NCT01803607	-		Terminated(Study halted premat... 展开 >>urely due to low enrollment.) 收起 <<	-	-
NCT01512667	Renal Insufficiency	Phase 1	Completed	-	-
NCT01512667	-		Completed	-	-
NCT01803607	Osteoporosis	Phase 3	Terminated(Study halted premat... 展开 >>urely due to low enrollment.) 收起 <<	-	-
NCT01120600	-		Completed	-	-

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

Odanacatib 纯度/质量文件产品仅供科研

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Odanacatib 生物活性

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Odanacatib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Odanacatib 质控信息

Odanacatib 生物活性

Odanacatib 动物研究

Odanacatib 临床研究

Odanacatib 参考文献

Odanacatib 实验方案

Odanacatib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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