Emricasan (IDN-6556)

製品コードS7775 バッチS777509

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 25 mg/mL (43.89 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) は、強力な不可逆的パンカスパーゼ阻害剤です。Emricasanはジカウイルス感染症の阻害剤です。
in vitro Emricasan (IDN-6556), also called PF-03491390, is an inhibitor of activated caspases with sub- to nanomolar activity in vitro. It shows neuroprotective activity for hNPCs but does not suppress ZIKV replication.
in vivo In the murine NASH model, stellate cell activation and hepatic fibrogenesis are attenuated by administration of Emricasan (IDN-6556), a pan-caspase inhibitor. It decreases liver injury but not metabolic derangement in NASH and also ameliorates inflammation. This compound is currently being evaluated in phase 2 clinical trials for the reduction of hepatic injury and liver fibrosis caused by chronic HCV infection.

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 (IDN-6556), or a combination of 92 μM PHA-690509 and this compound 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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/24750664/
  • https://pubmed.ncbi.nlm.nih.gov/27571349/

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:

SIGLEC12 mediates plasma membrane rupture during necroptotic cell death [ Nature, 2025, 10.1038/s41586-025-09741-1] PubMed: 41225007
Inhibition of heme biosynthesis triggers cuproptosis in acute myeloid leukemia [ Cell, 2025, S0092-8674(25)01233-4] PubMed: 41265435
WNK1 mediates M-CSF-induced macropinocytosis to enforce macrophage lineage fidelity [ Nat Commun, 2025, 16(1):4945] PubMed: 40436823
RIPK1 autophosphorylation at S161 mediates cell death and inflammation [ J Exp Med, 2025, 222(12)e20250279] PubMed: 40996439
IFNγ augments TKI efficacy by alleviating protein unfolding stress to promote GSDME-mediated pyroptosis in hepatocellular carcinoma [ Cell Death Dis, 2025, 16(1):512] PubMed: 40645933
Establishment of bovine extraembryonic endoderm stem cells enables efficient blastoid formation [ Cell Rep, 2025, 44(6):115707] PubMed: 40402743
Pan-caspase inhibitors induce secretion of HIV-1 latency reversal agent lymphotoxin-alpha from cytokine-primed NK cells [ Cell Death Discov, 2025, 11(1):44] PubMed: 39905001
Caspase cleavage of Kaposi sarcoma-associated herpesvirus proteins: a role for K5 in preventing caspase-mediated cell death during lytic replication [ J Virol, 2025, 99(9):e0062225] PubMed: 40882004
Neuroligin-3 R451C induces gain-of-function gene expression in astroglia in an astroglia-enriched brain organoid model [ Cell Regen, 2025, 14(1):1] PubMed: 39775628
Morphogen-guided neocortical organoids recapitulate regional areal identity and model neurodevelopmental disorder pathology [ bioRxiv, 2025, 2025.09.02.672952] PubMed: 40950130

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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