Emricasan (IDN-6556)

製品コードS7775 バッチS777506

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
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 (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[2].
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[1]. 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[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 (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
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
Protocol for purifying primitive neural progenitors by fractional passaging to generate astroglia-enriched cerebral organoid [ STAR Protoc, 2025, 6(4):104142] PubMed: 41091601

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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