CA-074 | Cathepsin B Inhibitor | AmBeed-信号通路专用抑制剂

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CA-074 {[allProObj[0].p_purity_real_show]}

货号：A976403

CA 074 is an inhibitor of cathepsin B with Ki of 2 - 5 nM.

CA-074 化学结构
CAS号：134448-10-5

CA-074 3D分子结构
CAS号：134448-10-5

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CA-074 纯度/质量文件产品仅供科研

货号：A976403 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: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

CA-074 生物活性

描述

Cathepsin B is a lysosomal cysteine protease of the papain family. It functions in intracellular protein catabolism and in certain situations may also be involved in other physiological processes, such as processing of antigens in the immune response, hormone activation and bone turnover. Cathepsin B is implicated in the pathology of chronic inflammatory diseases of airways and joints, and in cancer and pancreatitis^[1]. CA-074 inhibits cathepsin B with a Ki of 2 to 5 nM, whereas the initial Kis for cathepsin H and L are about 40-200 μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L.Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity^[2].CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug^[3].Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys^[4].

CA-074 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
NCT00856661	Stroke	Phase 3	Terminated(The recruitment int... 展开 >>o DIAS4 has been stopped as the result of DIAS 3 indicates that the study is unlikely to reach its primary endpoint with the current protocol) 收起 <<	-	-
NCT02585934	Alzheimer's Disease	Phase 3	Completed	-	-
NCT02723240	Cancer	Phase 1	Recruiting	June 30, 2019	United Kingdom ... 展开 >> Belfast City Hospital Not yet recruiting Belfast, United Kingdom, BT9 7AB Principal Investigator: Richard H Wilson, MD Beatson, West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom, G12 OYN Principal Investigator: Jeffry Evans, MD, FRCP Oxford University Hospitals NHS Trust Recruiting Oxford, United Kingdom, OX3 7LE Principal Investigator: Sarah P Blagden, Phd, FRCP 收起 <<

CA-074 参考文献

[1]J S Mort , D J Buttle. Int J Biochem Cell Biol. 1997 May;29(5):715-20.

[2]Towatari T, et al. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5.

[3] Montaser M, et al. CA-074, but not its methyl ester CA-074Me, is a selective inhibitor of cathepsin B within living cells. Biol Chem. 2002 Jul-Aug;383(7-8):1305-8.

[4] Yamashima T, et al. Inhibition of ischaemic hippocampal neuronal death in primates with cathepsin B inhibitor CA-074: a novel strategy for neuroprotection based on 'calpain-cathepsin hypothesis'. Eur J Neurosci. 1998 May;10(5):1723-33.

CA-074 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.61mL

0.52mL

0.26mL

13.04mL

2.61mL

1.30mL

26.08mL

5.22mL

2.61mL

CA-074 技术信息

CAS号	134448-10-5
分子式	C₁₈H₂₉N₃O₆
分子量	383.44

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 120 mg/mL(312.96 mM)，配合低频超声助溶，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

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

NCT00856661	Stroke	Phase 3	Terminated(The recruitment int... 展开 >>o DIAS4 has been stopped as the result of DIAS 3 indicates that the study is unlikely to reach its primary endpoint with the current protocol) 收起 <<	-	-
NCT02585934	Alzheimer's Disease	Phase 3	Completed	-	-
NCT02723240	Cancer	Phase 1	Recruiting	June 30, 2019	United Kingdom ... 展开 >> Belfast City Hospital Not yet recruiting Belfast, United Kingdom, BT9 7AB Principal Investigator: Richard H Wilson, MD Beatson, West of Scotland Cancer Centre Recruiting Glasgow, United Kingdom, G12 OYN Principal Investigator: Jeffry Evans, MD, FRCP Oxford University Hospitals NHS Trust Recruiting Oxford, United Kingdom, OX3 7LE Principal Investigator: Sarah P Blagden, Phd, FRCP 收起 <<
NCT01488240	Burn Scar	Not Applicable	Recruiting	June 2019	Canada, Manitoba ... 展开 >> University of Manitoba Recruiting Winnipeg, Manitoba, Canada, R3A 1R9 Contact: Justin P Gawaziuk, MSc 2047873669 jgawaziuk@hsc.mb.ca Principal Investigator: Sarvesh Logsetty, MD 收起 <<
NCT02542826	Pulmonary Disease, Chronic Obs... 展开 >>tructive 收起 <<	Not Applicable	Recruiting	August 2018	Canada, Quebec ... 展开 >> McConnell Centre for Innovative Medicine, Research Institute of the McGill University Health Centre Recruiting Montreal, Quebec, Canada, H4A 3J1 Contact: Dennis Jensen, Ph.D. 514-398-4184 ext 0541 dennis.jensen@mcgill.ca Principal Investigator: Dennis Jensen, Ph.D. 收起 <<
NCT03063424	Exercise Induced Bronchospasm	Not Applicable	Recruiting	December 2017	Canada, Quebec ... 展开 >> Université de Sherbrooke Recruiting Sherbrooke, Quebec, Canada, J1G2E8 Contact: Katia Carle-Talbot, MD, resident 514-592-1113 ext pag 0477 katia.carle-talbot@usherbrooke.ca Contact: Brian Grondin-Beaudoin, MD 819-346-1110 ext 14252 Brian.Grondin.Beaudoin@USherbrooke.ca 收起 <<
NCT02585934	-		Completed	-	-
NCT01835015	Age-related Macular Degenerati... 展开 >>on 收起 <<	Phase 1	Completed	-	-
NCT01978184	Pancreatic Cancer	Phase 2	Active, not recruiting	November 2018	United States, Pennsylvania ... 展开 >> Hillman Cancer Center Pittsburgh, Pennsylvania, United States, 15232 收起 <<
NCT00856661	-		Terminated(The recruitment int... 展开 >>o DIAS4 has been stopped as the result of DIAS 3 indicates that the study is unlikely to reach its primary endpoint with the current protocol) 收起 <<	-	-
NCT01835015	-		Completed	-	-
NCT00730301	Emphysema Chr... 展开 >>onic Obstructive Pulmonary Disease 收起 <<	Phase 4	Unknown	-	Austria ... 展开 >> Otto Wagner Hospital Recruiting Vienna, Austria, 1140 Contact: Arschang Valipour, MD arschang.valipour@wienkav.at Belgium University Antwerp Recruiting Antwerp, Belgium Contact: Paul Germonpre, MD Paul.Germonpre@uza.be Principal Investigator: Paul Germonpre, MD University Brussels Recruiting Brussels, Belgium Contact: Marc Meysman, MD Marc.Meysman@uzbrussel.be Principal Investigator: Marc Meysman, MD 收起 <<
NCT03646149	-		Enrolling by invitation	August 19, 2019	United States, California ... 展开 >> VA Greater Los Angeles Healthcare System, West Los Angeles, CA West Los Angeles, California, United States, 90073 收起 <<
NCT00057135	Schizophrenia ... 展开 >> Schizoaffective Disorder Bipolar Disorder 收起 <<	Not Applicable	Completed	-	United States, California ... 展开 >> VA San Diego Healthcare System, San Diego, CA San Diego, California, United States, 92161 United States, Illinois Edward Hines Jr. VA Hospital, Hines, IL Hines, Illinois, United States, 60141-5000 United States, Massachusetts East Orange Campus of the VA New Jersey Health Care System, East Orange, NJ East Orange, Massachusetts, United States, 07018 United States, Michigan VA Ann Arbor Healthcare System, Ann Arbor, MI Ann Arbor, Michigan, United States, 48105 United States, Rhode Island John D. Dingell VA Medical Center, Detroit, MI Detroit, Rhode Island, United States, 48201 收起 <<

CA-074 {[allProObj[0].p_purity_real_show]}

CA-074 纯度/质量文件产品仅供科研

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CA-074 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

CA-074 质控信息

CA-074 生物活性

CA-074 临床研究

CA-074 参考文献

CA-074 实验方案

CA-074 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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