Emricasan是一种口服有效、不可逆的广谱胱天蛋白酶抑制剂，具有良好的药代动力学特征。
Cas No.:254750-02-2
Sample solution is provided at 25 µL, 10mM.
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Emricasan is an orally active, irreversible, broad-spectrum caspase inhibitor with good pharmacokinetic profile [1]. Emricasan inhibits Zika virus (ZIKV) infection and suppresses infection-induced caspase-3 activity, leading a reduction in cell death[2]. Emricasan has been widely used in mouse models of liver injury to inhibit liver fibrosis and restore liver function[3].
In vitro, Emricasan treatment for 72h significantly inhibited the cell death induced by the ZIKV virus strains FSS13025 and PRVABC59 in the SNB-19 cells, with IC50 values of 0.84μM and 0.45μM, respectively[4]. Treatment with 10μM Emricasan for 72 hours significantly inhibited the cytotoxicity of HEI-OC1 cells induced by cisplatin[5]. Pre-treatment with 5μM Emricasan for 30 minutes can enhance the cell-killing effect of birinapant on MLL-AF9 cells and increase the expression of TNF[6].
In vivo, Emricasan treatment via oral administration at a dose of 10mg/kg/day for 7 consecutive days significantly inhibited hepatocyte death in late-stage liver cirrhosis rats and improved liver function, alleviating portal hypertension and liver microvascular dysfunction[7]. Intragastric administration of Emricasan at a single dose of 15mg/kg 15 minutes before ischemia alleviated cerebral IS/reperfusion injury in rats and reduced the infarct area[8].
References:
[1] Lekakis V, Cholongitas E. The impact of emricasan on chronic liver diseases: current data[J]. Clinical Journal of Gastroenterology, 2022, 15(2): 271-285.
[2] Da Silva S, Oliveira Silva Martins D, Jardim A C G. A review of the ongoing research on Zika virus treatment[J]. Viruses, 2018, 10(5): 255.
[3] Lekakis V, Cholongitas E. The impact of emricasan on chronic liver diseases: current data[J]. Clinical Journal of Gastroenterology, 2022, 15(2): 271-285.
[4] Xu M, Lee E M, Wen Z, et al. Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen[J]. Nature medicine, 2016, 22(10): 1101-1107.
[5] Nassauer L, Schott J W, Harre J, et al. The caspase-inhibitor Emricasan efficiently counteracts cisplatin-and neomycin-induced cytotoxicity in cochlear cells[J]. Journal of Molecular Medicine, 2024, 102(9): 1163-1174.
[6] Brumatti G, Ma C, Lalaoui N, et al. The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia[J]. Science translational medicine, 2016, 8(339): 339ra69-339ra69.
[7] Gracia‐Sancho J, Manicardi N, Ortega‐Ribera M, et al. Emricasan ameliorates portal hypertension and liver fibrosis in cirrhotic rats through a hepatocyte‐mediated paracrine mechanism[J]. Hepatology communications, 2019, 3(7): 987-1000.
[8] Tian J, Guo S, Chen H, et al. Combination of emricasan with ponatinib synergistically reduces ischemia/reperfusion injury in rat brain through simultaneous prevention of apoptosis and necroptosis[J]. Translational Stroke Research, 2018, 9(4): 382-392.
Emricasan是一种口服有效、不可逆的广谱胱天蛋白酶抑制剂，具有良好的药代动力学特征[1]。Emricasan抑制Zika病毒（ZIKV）感染，并抑制感染诱导的caspase-3活性，从而减少细胞死亡[2]。Emricasan已被广泛用于肝损伤小鼠模型，以抑制肝纤维化和恢复肝功能[3]。
在体外，Emricasan处理72小时显著抑制了ZIKV毒株FSS13025和PRVABC59在SNB-19细胞中诱导的细胞死亡，IC50值分别为0.84µM和0.45µM[4]。使用10µM的Emricasan处理72小时，显著抑制了顺铂诱导的HEI-OC1细胞的细胞毒性[5]。使用5µM的Emricasan预处理30分钟，可增强birinapant对MLL-AF9细胞的杀伤作用，并增加TNF的表达[6]。
在体内，每日口服给予10mg/kg剂量Emricasan，连续7天，显著抑制了晚期肝硬化大鼠的肝细胞死亡，改善了肝功能，缓解了门静脉高压和肝脏微血管功能障碍[7]。在缺血前15分钟单次灌胃给予15mg/kg剂量的Emricasan，减轻了大鼠脑缺血/再灌注损伤，并减少了梗死面积[8]。
| Cell experiment [1]: | |
Cell lines | HEI-OC1 cells |
Preparation Method | HEI-OC1 cells were cultured under permissive conditions (33°C and 10% CO2) in high-glucose Dulbecco's modified Eagle's medium (DMEM) with 10% heat-inactivated fetal bovine serum, 100U/ml penicillin, and 1mM sodium pyruvate. 2×103 cells were seeded into 96-well plates for 24h. The MV4-11 cells were cultured under the conditions of 37°C, 10% CO2 and humidity in RPMI medium supplemented with 10% fetal bovine serum. In the presence of Emricasan (10μM), the cells are treated with cisplatin (5μM) for 72 hours, and then the cell viability is analyzed. |
Reaction Conditions | 10μM; 72h |
Applications | Emricasan treatment reduced cell death of HEI-OC1 cells caused by cisplatin. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | By inducing chronic inhalation of carbon tetrachloride (CCl4) and simultaneously adding phenobarbital to the drinking water, male Wistar rats were made to develop liver cirrhosis. When the rats developed ascites (approximately 12-14 weeks later), the toxicant administration was stopped, and treatment was initiated one week later. The liver cirrhosis rats were respectively treated with Emricasan (10mg/kg/day; p.o.) or the vehicle (0.9% dimethylcarboxycellulose; p.o.) for 7 days, and the rat livers were collected for analysis. |
Dosage form | 10mg/kg/day for 7 days; p.o. |
Applications | Emricasan treatment improved liver function, alleviating portal hypertension and liver microvascular dysfunction in the cirrhotic rats. |
References: | |
| Cas No. | 254750-02-2 | SDF | |
| 别名 | 恩利卡生; PF 03491390; IDN-6556 | ||
| Canonical SMILES | FC1=C(C(F)=C(C=C1F)F)OCC([C@@H](NC([C@@H](NC(C(NC2=C(C=CC=C2)C(C)(C)C)=O)=O)C)=O)CC(O)=O)=O | ||
| 分子式 | C26H27F4N3O7 | 分子量 | 569.5 |
| 溶解度 | DMSO: ≥ 42 mg/mL (73.75 mM) | 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 | 1.7559 mL | 8.7796 mL | 17.5593 mL |
| 5 mM | 351.2 μL | 1.7559 mL | 3.5119 mL |
| 10 mM | 175.6 μL | 878 μL | 1.7559 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% Appearance: A solid
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