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.
For research use only. We do not sell to patients.
- Purity : 99.31%
- Formula: C114H156N24O28.xC2HF3O2
- Molecular Weight:2310.60 (free base)
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Storage:
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HIF-1α |
In Vitro
In thioglycolate-elicited C57BL/6 peritoneal macrophages, APL180 (50 µg/mL; overnight) suppresses M1 inflammatory/glycolytic markers and augments HIF-2α in M1-polarized cells without affecting M2-polarized HIF-2α[2].
In RAW 264.7 mouse macrophages, APL180 (50 µg/mL; overnight) suppresses M1-associated iNOS/CCL3 and glycolytic/HIF-1α markers while upregulating CD206 and arginase in M1-polarized cells[2].
APL180 (150-1,000 ng/mL) ex vivo dose-dependently improves the HII in human plasma samples, with 150 ng/mL sufficient to sequester most HII-affecting oxidized lipids[1].
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.
In Vivo
APL180 (100 µg/day; i.v. via tail vein; once daily; 5 consecutive days) TFA does not alter cardiac function or monocyte/macrophage profiles in sham-operated mice[2].
APL180 (5 mg/kg; i.p.; before ethanol gavages) TFA does not produce behavioural changes in female Wistar rats subjected to alcohol binge drinking[3].
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.
Chemical Information
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Appearance Solid
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Molecular Weight 2310.60 (free base)
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Formula C114H156N24O28.xC2HF3O2
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Color White to off-white
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Synonyms
L-4F TFA
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Sequence
Ac-Asp-Trp-Phe-Lys-Ala-Phe-Tyr-Asp-Lys-Val-Ala-Glu-Lys-Phe-Lys-Glu-Ala-Phe-NH2
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Sequence Shortening
Ac-DWFKAFYDKVAEKFKEAF-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
In Vivo:
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.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
APL180 TFA Related Classifications
HY-P6365 Related Classifications
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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