Emricasan (IDN-6556)

製品コードS7775 バッチS777504

印刷

化学情報

Chemical Structure Synonyms PF 03491390, PF-03491390 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H27F4N3O7
分子量 569.50 CAS No. 254750-02-2
Solubility (25°C)* 体外 DMSO 100 mg/mL (175.59 mM)
Ethanol 100 mg/mL (175.59 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.
in vitro Emricasan, also called IDN-6556 or PF-03491390, is an inhibitor of activated caspases, and it has sub- to nanomolar activity in vitro. Emricasan shows neuroprotective activity for hNPCs but does not suppress ZIKV replication[2].
in vivo Emricasan decreases liver injury but not metabolic derangement in NASH. It also ameliorates inflammation. In the murine NASH model, stellate cell activation and hepatic fibrogenesis are attenuated by administration of the pan-caspase inhibitor Emricasan[1]. Emricasan is currently being evaluated in phase 2 clinical trials for the reduction of hepatic injury and liver fibrosis caused by chronic HCV infection[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Astrocytes
濃度 9 μM
反応時間 1 h
実験の流れ Astrocytes are mock-infected, treated with DMSO or treated with 2 μM niclosamide, 92 μM PHA-690509, 9 μM emricasan, or a combination of 92 μM PHA-690509 and 9 μM emricasan for 1 h before infection with PRVABC59 (MOI = 0.5). Cells are fixed 24 h after infection and stained for ZIKVE and nuclei.
動物実験 動物モデル C57BL/6J mice
投薬量 0.3mg/kg/day
投与方法 i.g.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The RIPK1 death domain restrains ZBP1- and TRIF-mediated cell death and inflammation [ Immunity, 2024, S1074-7613(24)00221-8] PubMed: 38744293
Neuronal STING activation in amyotrophic lateral sclerosis and frontotemporal dementia [ Acta Neuropathol, 2024, 147(1):56] PubMed: 38478117
ZBP1 causes inflammation by inducing RIPK3-mediated necroptosis and RIPK1 kinase activity-independent apoptosis [ Cell Death Differ, 2024, 31(7):938-953] PubMed: 38849574
Caspase cleavage of RIPK3 after Asp333 is dispensable for mouse embryogenesis [ Cell Death Differ, 2024, 31(2):254-262.] PubMed: 38191748
Hepatocyte-macrophage crosstalk via the PGRN-EGFR axis modulates ADAR1-mediated immunity in the liver [ Cell Rep, 2024, 43(7):114400] PubMed: 38935501
Craniofacial chondrogenesis in organoids from human stem cell-derived neural crest cells [ iScience, 2024, 27(4):109585] PubMed: 38623327
Anti-apoptotic treatment of warm ischemic male rat livers in machine perfusion improves symptoms of ischemia-reperfusion injury [ Heliyon, 2024, 10(8):e29519] PubMed: 38660283
Regenerative human liver organoids (HLOs) in a pillar/perfusion plate for hepatotoxicity assays [ bioRxiv, 2024, 2024.03.25.586638] PubMed: 38586058
Reproducible generation of human liver organoids (HLOs) on a pillar plate platform via microarray 3D bioprinting [ bioRxiv, 2024, 2024.03.11.584478] PubMed: 38559126
Synaptic plasticity in human thalamocortical assembloids [ bioRxiv, 2024, 2024.02.01.578421] PubMed: 38352415

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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