Emricasan
(Synonyms: 恩利卡生; PF 03491390; IDN-6556) 目录号 : GC35980
A pan-caspase inhibitor
Cas No.:254750-02-2
Sample solution is provided at 25 µL, 10mM.
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Emricasan is a pan-caspase inhibitor.1,2,3,4 Ex vivo, emricasan (10 mg/kg) prevents cold ischemia-warm reperfusion-induced sinusoidal endothelial cell (SEC) apoptosis and inhibits caspase-3 activation in rat liver by 55 and 94%, respectively.1 In vivo, emricasan reduces alanine aminotransferase (ALT) levels (ED50s = <0.01-0.38 mg/kg) as well as apoptosis and caspase activity in a dose-dependent manner in the α-Fas mouse and D-Gln/LPS rat models of liver injury.2 Emricasan reduces caspase-3 and caspase-8 activity, serum ALT levels, hepatocyte apoptosis, and hepatic fibrogenesis in a mouse model of high-fat diet-induced non-alcoholic steatohepatitis (NASH).3 It also enhances islet engraftment and lowers post-transplant fasting glucose levels in a porcine islet autotransplant model.4
1.Natori, S., Higuchi, H., Contreras, P., et al.The caspase inhibitor IDN-6556 prevents caspase activation and apoptosis in sinusoidal endothelial cells during liver preservation injuryLiver Transpl.9(3)278-284(2003) 2.Hoglen, N.C., Chen, L.S., Fisher, C.D., et al.Characterization of IDN-6556 (3-[2-(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid): A liver-targeted caspase inhibitorJ. Pharmacol. Exp. Ther.309(2)634-640(2004) 3.Barreyro, F.J., Holod, S., Finocchietto, P.V., et al.The pan-caspase inhibitor emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitisLiver Int.35(3)953-966(2015) 4.McCall, M.D., Maciver, A.M., Kin, T., et al.Caspase inhibitor IDN6556 facilitates marginal mass islet engraftment in a porcine islet autotransplant modelTransplantation94(1)30-35(2012)
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Animal experiment: |
Mice[2] The male C57BL/6J mice are age-matched and used at approximately 12-16 weeks of age. Four groups are studied (n=60) with 15 mice per group. Groups 1 and 3 receive regular chow. Groups 2 and 4 receive HFD and 50 g/L (Sucrose) is added to drinking water for 20 weeks. Groups 3 and 4 receive Emricasan 0.3 mg/kg/day per os, and Group 1 and 2 receive the vehicle. The oral administration of Emricasan at doses of 0.3 mg/kg corresponds to the ED90 value to prevent liver injury in the model of α-Fas-induced liver injury. Total body weight is measured at 0, 5, 10, 15 and 20 weeks. Rats[3] The male Sprague-Dawley rats are cannulated in the carotid artery under isoflurane anesthesia and allowed to recover for at least 1 day before drug administration. Blood (100 μL/sample) is taken from the carotid cannula 2 to 240 min after administration of Emricasan (i.v., s.c., p.o., or i.p.). Serum is prepared and frozen immediately until analysis. In studies measuring drug concentrations in portal and systemic blood, individual rats are bled (three animals per time point) simultaneously from the portal vein and inferior vena cava. In the biliary excretion study, bile is collected from the common bile duct after i.v. and p.o. administration of Emricasan (10 mg/kg) over a 24-h period on ice and frozen until analysis. |
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References: [1]. Gracia-Sancho J, et al. Emricasan Ameliorates Portal Hypertension and Liver Fibrosis in Cirrhotic Rats Through a Hepatocyte-Mediated Paracrine Mechanism. Hepatol Commun. 2019 Apr 22;3(7):987-1000. |
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| 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 | 0.3512 mL | 1.7559 mL | 3.5119 mL |
| 10 mM | 0.1756 mL | 0.878 mL | 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet