FPS-ZM1

製品コードS8185 バッチS818502

印刷

化学情報

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

C20H22ClNO

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)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
3.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% Corn oil
3.25mg/ml Taking the 1 mL working solution as an example, add 50 μL of 65 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 CHO cells
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.

動物実験 動物モデル C57BL/6 mice
投薬量 1 mg/kg
投与方法 i.v.

カスタマーフィードバック

, , 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]

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 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。