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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C20H22ClNO |
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分子量 | 327.85 | CAS No. | 945714-67-0 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 66 mg/mL (201.31 mM) | ||||||||
Ethanol | 66 mg/mL (201.31 mM) | ||||||||||
Water | Insoluble | ||||||||||
体内 (毎回新しく調製した物を用意してください) |
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* <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. |
製品説明 | FPS-ZM1 is a blood-brain-barrier permeant, non-toxic, tertiary amide compound which is a high affinity RAGE-specific inhibitor, blocking Aβ binding to the V domain of RAGE. |
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in vitro | FPS-ZM1 blocks Aβ binding to the V domain of RAGE and inhibited Aβ40- and Aβ42-induced cellular stress in RAGE-expressing cells in vitro. It blocks binding of other ligands to RAGE as well, such as S100B, AGE, and HMGB1, which have been suggested to contribute to RAGE-mediated long-term tissue damage in models of diabetes, immune/inflammatory disorders, and AD[1]. |
in vivo | FPS-ZM1 is nontoxic to mice and readily crossed the blood-brain barrier (BBB).It effectively controls progression of an Aβ-mediated brain disorder and the related neurovascular and cognitive dysfunction in 17-month-old APPsw/0 mice with fully developed Aβ and amyloid pathology by blocking RAGE actions at the BBB and in brain. Also, FPS-ZM1 blocks RAGE-dependent BACE1 expression and activity in brain of 17-month-old APPsw/0 mice[1]. |
細胞アッセイ | 細胞株 | CHO cells |
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濃度 | 10 nM to 10 μM | |
反応時間 | 72 h | |
実験の流れ | CHO cells are treated for 72 hours with different concentrations of inhibitors ranging from 10 nM to 10 μM. The cellular toxicity was determined using the WST-8 Assay Kit. |
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動物実験 | 動物モデル | C57BL/6 mice |
投薬量 | 1 mg/kg | |
投与方法 | i.v. |
, , Biochem Biophys Res Commun, 2017, 495(1):78-85
Data from [Data independently produced by , , Int Immunopharmacol, 2018, 59:187-196]
Data from [Data independently produced by , , International Immunopharmacology, 2018, 59:187-196]
The critical role of RAGE in severe influenza infection: A target for control of inflammatory response in the disease [ Clin Immunol, 2024, 262:110178] | PubMed: 38460892 |
Circulating extracellular vesicles from patients with traumatic brain injury induce cerebrovascular endothelial dysfunction [ Pharmacol Res, 2023, 192:106791] | PubMed: 37156450 |
The TRIM21-FOXD1-BCL-2 axis underlies hyperglycaemic cell death and diabetic tissue damage [ Cell Death Dis, 2023, 14(12):825] | PubMed: 38092733 |
RAGE inhibition blunts insulin-induced oncogenic signals in breast cancer [ Breast Cancer Res, 2023, 25(1):84] | PubMed: 37461077 |
Effects of HMGB1/RAGE/cathespin B inhibitors on alleviating hippocampal injury by regulating microglial pyroptosis and caspase activation in neonatal hypoxic-ischemic brain damage [ J Neurochem, 2023, 167(3):410-426] | PubMed: 37753942 |
Proinflammatory S100A9 Stimulates TLR4/NF-κB Signaling Pathways Causing Enhanced Phagocytic Capacity of Microglial Cells [ Immunol Lett, 2023, 255:54-61] | PubMed: 36870421 |
Stratification of radiosensitive brain metastases based on an actionable S100A9/RAGE resistance mechanism [ Nat Med, 2022, 28(4):752-765] | PubMed: 35411077 |
S100A9-CXCL12 activation in BRCA1-mutant breast cancer promotes an immunosuppressive microenvironment associated with resistance to immunotherapy [ Nat Commun, 2022, 13(1):1481] | PubMed: 35304461 |
Elevated neutrophil extracellular traps by HBV-mediated S100A9-TLR4/RAGE-ROS cascade facilitate the growth and metastasis of hepatocellular carcinoma [ Cancer Commun (Lond), 2022, 10.1002/cac2.12388] | PubMed: 36346061 |
RAGE promotes dysregulation of iron and lipid metabolism in alcoholic liver disease [ Redox Biol, 2022, 59:102559] | PubMed: 36502724 |
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。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。