CA-074 Me
(Synonyms: L-TRANS-环氧琥珀酸-ILE-PRO-OME丙醛,CA-074Me) 目录号 : GC15917
CA-074 Me（CA-074甲酯）是组织蛋白酶B（CB）的特异性抑制剂。
Cas No.:147859-80-1
Sample solution is provided at 25 µL, 10mM.
CA-074 Me (CA-074 methyl ester) is a specific inhibitor of Cathepsin B(CB)[1-5].
CA-074 Me pretreated 2h with a range of doses can protect lethal toxin-sensitive macrophages from cell death and prevents the activation of caspase-1[1]. CA-074 Me(5μM and 50μM,48h) also inhibits RANK-ligand induced osteoclastogenesis in bone marrow-derived monocyte cells[2].CA-074 Me (20μM, 24h), also partially attenuated free fatty acid induced apoptosis[3].
CA-074 Me (4mg/kg/day, 7day, i.m.) reduced CB expression,decreased inflammation score and attenuated apoptosis in muscle tissues of the guinea-pig model of CVB1-induced polymyositis[4]. CA-074 Me (1μg, 1h, intracerebroventricularly) pretreatment inhibits lysosomal membrane rupture induced by 20-min global cerebral ischemia/reperfusion injury in Sprague-Dawley rats[5].
References:
[1] Newman Z L, Leppla S H, Moayeri M. CA-074 Me protection against anthrax lethal toxin[J]. Infection and immunity, 2009, 77(10): 4327-4336.
[2] Patel N, Nizami S, Song L, et al. CA-074 Me compound inhibits osteoclastogenesis via suppression of the NFATc1 and c‐FOS signaling pathways[J]. Journal of Orthopaedic Research, 2015, 33(10): 1474-1486..
[3] Wu X, Zhang L, Gurley E, et al. Prevention of free fatty acid-induced hepatic lipotoxicity by 18β-glycyrrhetinic acid through lysosomal and mitochondrial pathways[J]. Hepatology, 2008, 47(6): 1905-1915.
[4] Feng Y, Ni L, Wang Q. Administration of cathepsin B inhibitor CA-074 Me reduces inflammation and apoptosis in polymyositis[J]. Journal of dermatological science, 2013, 72(2): 158-167.
[5] Xu Y, Wang J, Song X, et al. Protective mechanisms of CA074-me (other than cathepsin-B inhibition) against programmed necrosis induced by global cerebral ischemia/reperfusion injury in rats[J]. Brain Research Bulletin, 2016, 120: 97-105.
CA-074 Me（CA-074甲酯）是组织蛋白酶B（CB）的特异性抑制剂[1-5]。
CA-074 Me预处理2小时，在一定剂量范围内CA-074 Me可保护致命毒素敏感巨噬细胞免于细胞死亡，并阻止caspase-1的激活[1]。CA-074 Me（5μM和50μM，48小时）还可抑制骨髓来源的单核细胞中RANK配体诱导的破骨细胞生成[2]。CA-074 Me（20μM, 24小时）也能部分减弱游离脂肪酸诱导的细胞凋亡[3]。
CA-074 Me（4mg/kg/天，7天，肌肉注射）降低了豚鼠CVB1诱发的多发性肌炎模型中肌肉组织中的CB表达，降低炎症评分，并减轻细胞凋亡[4]。CA-074 Me（1μg，1小时，侧脑室注射）预处理可抑制Sprague-Dawley大鼠20分钟全脑缺血/再灌注损伤引起的溶酶体膜破裂[5]。
| Cell experiment [1]: | |
Cell lines | Bone marrow-derived macrophages and RAW 264.7 |
Preparation Method | Macrophages were grown in 96-well plates to 90% confluence. All cells were pretreated with CA-074 Me or vehicle (dimethyl sulfoxide) at the indicated concentrations for various lengths of time and then treated with lethal toxin (LT) (1g/ml) for 2.5h. Viability was assessed by addition of MTT. |
Reaction Conditions | 100~500μM; 2h |
Applications | CA-074 Me treatment protects against LT-induced macrophage death. |
| Animal experiment [2]: | |
Animal models | guinea-pig model of CVB1-induced polymyositis (PM) |
Preparation Method | CA-074 Me (4mg/kg/day, i.m.) was given 24h after Coxsackie virus B1 (CVB1) injection for 7 consecutive days. Four experimental groups were included: (A) Sham (Healthy) group: received normal saline (NS); (B) CVB group: received CVB1 + FCA; (C) NS group (pseudo intervention group): received CVB1 + FCA + NS; and (D) CA-074 Me group: CVB1 + FCA + CA-074 Me. Four weeks after CVB1 injection. |
Dosage form | 4mg/kg/day; 7days; i.m. |
Applications | CA-074 Me attenuated CVB1-induced increases in CB activity and expression, and reduced apoptosis, inflammation, and fibrosis in PM. |
References: | |
| Cas No. | 147859-80-1 | SDF | |
| 别名 | L-TRANS-环氧琥珀酸-ILE-PRO-OME丙醛,CA-074Me | ||
| 化学名 | methyl (2S)-1-[(2S)-3-methyl-2-[[(2S,3S)-3-(propylcarbamoyl)oxirane-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carboxylate | ||
| Canonical SMILES | CCCNC(=O)C1C(O1)C(=O)NC(C(C)CC)C(=O)N2CCCC2C(=O)OC | ||
| 分子式 | C19H31N3O6 | 分子量 | 397.5 |
| 溶解度 | ≥ 19.875mg/mL in DMSO, ≥ 51.5 mg/mL in EtOH with ultrasonic | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5157 mL | 12.5786 mL | 25.1572 mL |
| 5 mM | 0.5031 mL | 2.5157 mL | 5.0314 mL |
| 10 mM | 0.2516 mL | 1.2579 mL | 2.5157 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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