APL180
APL180 (L-4F) is an Apo-A1 mimetic peptide. APL180 binds oxidized/oxidizable lipids with high affinity and sequesters pro-inflammatory oxidized lipids. APL180 downregulates glycolysis-related genes and HIF-1α expression, and upregulates CD206 and Arginase. APL180 inhibits atherosclerotic lesion progression and platelet aggregation. APL180 attenuates adverse left ventricular remodeling and systolic dysfunction after myocardial infarction. APL180 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。
- CAS 番号: 388566-97-0
- 分子式: C114H156N24O28
- 分子量:2310.60
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 388566-97-0
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分子量 2310.60
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分子式 C114H156N24O28
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別名
L-4F
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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
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Keywords
- APL180
- 388566-97-0
- 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