中文名称: | 恩利卡生 | ||||
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英文名称: | Emricasan | ||||
别名: | N-[2-(叔丁基)苯基]-2-氧代甘氨酰-N-[(1S)-1-(羧基甲基)-2-氧代-3-(2,3,5,6-四氟苯氧基)丙基]-L-丙氨酰胺 IDN6556;PF03491390; (S)-3-((S)-2-(2-((2-(tert-butyl)phenyl)amino)-2-oxoacetamido)propanamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid | ||||
CAS No: | 254750-02-2 | 分子式: | C26H27F4N3O7 | 分子量: | 569.51 |
CAS No: | 254750-02-2 | ||||
分子式: | C26H27F4N3O7 | ||||
分子量: | 569.51 |
基本信息
产品编号:E10258 |
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产品名称:Emricasan |
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CAS: |
254750-02-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
569.51 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL (175.59mM) |
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Ethanol |
100mg/mL (175.59mM) |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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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。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
1.7559mL |
8.7796mL |
17.5593mL |
5mM |
0.3512mL |
1.7559mL |
3.5119mL |
10mM |
0.1756mL |
0.8780mL |
1.7559mL |
50mM |
0.0351mL |
0.1756mL |
0.3512mL |
生物活性
产品描述 |
一种口服有效的不可逆的pan-caspase抑制剂。 |
靶点/IC50 |
Caspase |
体外研究 |
Emricasan (PF 03491390; IDN-6556) (50μM; 24 hours) directly improves hepatocytes phenotype in primary rat cirrhotic hepatocytes.Emricasan (10-50μM) has hepatoprotective effects in human liver cells. |
体内研究 |
Emricasan (PF 03491390; IDN-6556) is orally active that is retained in the liver for prolonged period of time. TUNEL-positive cells are considerably increased by five-fold in mice fed a HFD and are reduced under Emricasan treatment. In accordance with this observation caspase-3 and -8 are increased in HFD-fed mice by 1.5- and 1.3-fold respectively and are significantly decreased by Emricasan treatment.When comparing efficacy by multiple routes of administration, Emricasan is administered i.p., p.o., i.m., or i.v. (0.03-3mg/kg). Caspase 3-like activities, measured as DEVD-AMC cleavage, dose dependently decreased with a 92.5% reduction after the highest dose of Emricasan (3mg/kg). Emricasan is initially tested in the α-Fas model of liver injury, marked hepatocellular apoptosis, and peak ALT activities within 6h. Emricasan is administered i.p. immediately after administration of α-Fas, ALT activities, measured 6h later, decreased in a dose-dependent manner with an ED50 value of 0.08 (0.06-0.12)mg/kg.Emricasan is a highly selective pan-caspase inhibitor demonstrating irreversible inhibition and a significant first-pass effect.In both syngeneic mouse islets and human islets transplanted into immunodeficient mice, Emricasan (i.p., 20mg/kg) given for 7 days post-transplant led to a significantly enhanced rate of diabetes reversal as compared to vehicle. |
推荐实验方法(仅供参考)
细胞实验: |
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细胞系 |
星形胶质细胞 |
浓度 |
9μM |
处理时间 |
1h |
方法 |
模拟感染星形胶质细胞,用DMSO或2μM niclosamide, 92μM PHA-690509, 9μM emricasan 或 92μM PHA-690509 和9μM emricasan结合使用,在感染PRVABC59前处理细胞1小时。感染细胞后24小时,收集并固定细胞。 |
动物实验: |
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Mice 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 50g/L (Sucrose) is added to drinking water for 20 weeks. Groups 3 and 4 receive Emricasan 0.3mg/kg/day per os, and Group 1 and 2 receive the vehicle.The oral administration of Emricasan at doses of 0.3mg/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. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )