APL180 TFA
Based on 1 Customer Validation
APL180 TFA (L-4F TFA) is an Apo-A1 mimetic peptide. APL180 TFA binds oxidized/oxidizable lipids with high affinity and sequesters pro-inflammatory oxidized lipids. APL180 TFA downregulates glycolysis-related genes and HIF-1α expression, and upregulates CD206 and Arginase. APL180 TFA inhibits atherosclerotic lesion progression and platelet aggregation. APL180 TFA attenuates adverse left ventricular remodeling and systolic dysfunction after myocardial infarction. APL180 TFA can be used for research on ovarian cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.31%
- 分子式: C114H156N24O28.xC2HF3O2
- 分子量:2310.60 (free base)
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
HIF-1α |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RAW 264.7 mouse macrophage cell line
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Concentration:50 µg/mL
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Incubation Time:overnight
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Result:L-4F significantly reduced expression of iNOS and CCL3 in M1-polarized RAW 264.7 cells.
L-4F significantly augmented expression of CD206 and arginase in M1-polarized RAW 264.7 cells compared with M0-polarized cells.
Significantly downregulated glycolytic gene and HIF-1α expression in M1-polarized cells.
Did not affect HIF-2α expression in M2-polarized macrophages.
体内実験
APL180 (100 µg/day; i.v. via tail vein; once daily; 5 consecutive days) does not alter cardiac function or monocyte/macrophage profiles in sham-operated mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 10-12 weeks of age)[2]
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Dosage:100 µg/day in 200 µL PBS
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Administration:i.v. via tail vein; once daily; 5 consecutive days
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Result:Echocardiography: L-4F prevented progressive LV chamber dilatation and dysfunction; changes in LV EDV, ESV, and EF from day 3 to day 8 were smaller than in PBS-treated MI mice.
Representative LV volumes: PBS 3 days post-MI 61 µL and 8 days post-MI 88 µL; L-4F 3 days post-MI 60 µL and 8 days post-MI 65 µL.
Blood: PBS-treated MI mice had nearly 3-fold increased Ly6Chi monocytes versus sham; L-4F suppressed Ly6Chi monocytosis to levels comparable to sham.
No significant L-4F-mediated effects on circulating Ly6Clow monocytes in MI mice.
Spleen: PBS-treated MI mice had ~2-fold increased frequency of pro-inflammatory Ly6Chi monocytes in the spleen at 8 days post-MI versus sham; L-4F suppressed and normalized this.
Augmented spleen weight in MI mice versus L-4F-treated sham-operated mice.
Heart macrophages: L-4F suppressed pro-inflammatory F4/80+Ly6Chi macrophages in post-MI hearts without significant effects on F4/80+Ly6Clow macrophages.
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Animal Model:C57BL/6J (male, 10-12 weeks of age)[2]
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Dosage:100 µg/day in 200 µL PBS
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Administration:i.v. via tail vein; once daily; 5 consecutive days
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Result:Echocardiography: no differences between pre-administration LV EDV, ESV, and EF; no meaningful changes in EDV, ESV, and EF over time after either L-4F or PBS administration.
Blood: circulating Ly6Chi and Ly6Clow monocytes were comparable regardless of group.
Heart macrophages: L-4F had no effect on macrophages in sham-operated hearts.
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Animal Model:Wistar (female, 200-225 g)[3]
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Dosage:5 mg/kg
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Administration:i.p.; 15 min before alcohol gavages
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Result:4F administration showed no behavioural changes.
Exogenous administration of the ApoAI mimetic peptide had no effect on alcohol binge drinking-induced alterations during abstinence.
化学情報
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性状 Solid
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分子量 2310.60 (free base)
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分子式 C114H156N24O28.xC2HF3O2
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Color White to off-white
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別名
L-4F TFA
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配列
Ac-Asp-Trp-Phe-Lys-Ala-Phe-Tyr-Asp-Lys-Val-Ala-Glu-Lys-Phe-Lys-Glu-Ala-Phe-NH2
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シーケンスの短縮
Ac-DWFKAFYDKVAEKFKEAF-NH2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (294 KB)
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SDS (252 KB)
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- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
APL180 TFA 関連分類
HY-P6365 関連分類
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Keywords
- APL180
- L-4F
- APL 180
- APL-180
- HIF/HIF Prolyl-Hydroxylase
- Arginase
- Apolipoprotein
- HDL inflammatory index inhibitor
- atherosclerotic lesion
- hematopoietic stem cell
- lipid sequestrant
- macrophage plasticity
- monocyte chemoattractant protein
- monocyte migration
- myocardial infarction
- ovarian cancer
- oxidized lipids
- Inhibitor
- inhibitor
- inhibit