计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
CA-074 methyl ester 是CA-074的细胞渗透性类似物，可作为不可逆的组织蛋白酶B抑制剂。据报道，CA-074甲酯在啮齿动物模型中抑制骨再吸收，并显示出在体外抑制B16黑素瘤细胞的侵袭。
介绍：
CA-074 methyl ester 是一种特异性的 Cathepsin B 抑制剂，具有保护神经，抗癌、抗炎等多种生物活性。
用途：
使用CA-074甲酯用作心肌细胞、HeLa细胞和胰腺癌PANC-1细胞中的组织蛋白酶B抑制剂。
Information
CA-074 methyl ester (CA-074 Me) CA-074 methyl ester (CA-074 Me, Cathepsin B Inhibitor IV) is a membrane-permeable derivative of CA-074 and acts as an irreversible cathepsin B inhibitor.
In vitro
CA-074Me is able to inhibit cathepsin L within living HL-60 cells and bloodstream forms of Trypanosoma brucei brucei, but does not inhibit cathepsin L in the absence of thiols. CA-074Me is converted into CA-074 by intracellular esterasesand is, therefore, able to inhibit cathepsin B in GSH-depleted HL-60 cell. It is suggested that CA-074 rather than CA-074Me should be used to selectively inhibit cathespsin B within living cells. Myotube size and number and induced levels of fusion-related creatine phosphokinase activity and myosin heavy-chain protein are reduced from 30 to 50% in CA074Me-treated myoblasts. These reductions are also dose related. Micromolar concentrations of CA074Me inhibit catB activity in differentiating myoblasts.
In vivo
Administration of CA074Me to the London APP mice results in significant improvement in memory deficit, reduces amyloid plaque load in brain, reduces levels of Aβ40 and Aβ42 in brain, and reduces C-terminal β-secretase fragment (CTFβ) derived from APP by β-secretase when compared with untreated control animals. It has no effect on any of these parameters in mice expressing the Swe mutant β-secretase site of APP (in Swedish/London APP mice). In vivo icv administration of CA074Me to normal guinea pigs results in substantial reduction of brain Aβ levels and inhibits β-secretase activity.
Cell Data
cell lines：Cultured human mast cells (CHMC)
Concentrations：100 μM
Incubation Time：2 h
Powder Purity:≥99%
规格
英文别名
Cathepsin B Inhibitor IV | L-Proline, N-[[(2S,3S)-3-[(propylamino)carbonyl]-2-oxiranyl]carbonyl]-L-isoleucyl-, methyl ester
规格或纯度
10mM in DMSO
英文名称
CA-074 methyl ester (CA-074 Me)
生化机理
CA-074 甲酯（CA-074 Me，Cathepsin B 抑制剂 IV）是 CA-074 的一种膜渗透性衍生物，是一种不可逆的 cathepsin B 抑制剂。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCCNC(=O)[C@@H]1[C@H](O1)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N2CCC[C@H]2C(=O)OC
分子量
397.47
Reaxy-Rn
25187464
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25187464&ln=
技术文档
高级数据
关联靶点（人）
CTSB
Tchem
组织蛋白酶B(Cathepsin B)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (109.38 mM); Ethanol: 100 mg/mL (109.38 mM); Water: Insoluble;
比旋光度
-33.3 - -12.1°c = 1.4 in EtOH, 20° C
安全和危险性（GHS）
WGK Germany
3
个人防护装备
Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter
RIDADR
NONHforallmodesoftransport
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
溶液计算器
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危险品化学品经营许可证（带存储）