| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Annexin A2 (AnxA2)[1]
LCKLSL hydrochloride targets annexin A2 (AnxA2), a calcium‑dependent phospholipid‑binding protein that plays a role in fibrinolysis, angiogenesis, and cell proliferation. It competitively inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. By blocking this interaction, it inhibits plasmin generation and has anti‑angiogenic activity. The compound also inhibits the development of experimental autoimmune encephalomyelitis (EAE) in mice. |
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| ln Vitro |
In hypoxic settings, LCKLSL hydrochloride (0–2 mg) therapy reduces plasmin generation and VEGF-induced tPA activity in human retinal microvascular endothelial cells (RMVEC) [1].
In vitro, LCKLSL hydrochloride potently inhibits the binding of tissue plasminogen activator (tPA) to AnxA2. It inhibits plasmin generation. The compound exhibits anti‑angiogenic activity. These activities confirm its role as a competitive AnxA2 inhibitor. |
| ln Vivo |
The application of LCKLSL hydrochloride resulted in the suppression of the angiogenic response in two in vivo models of angiogenesis: the mouse Matrigel plug assay and the chicken chorioallantoic membrane. Vessel length was dramatically reduced after receiving LCKLSL HCl peptide treatment. The number of vessel branches, junctions, and endpoints was considerably reduced by LCKLSL HCl peptide at a concentration of 5 μg/mL [1].
In vivo, LCKLSL hydrochloride inhibits the development of experimental autoimmune encephalomyelitis (EAE) in mice. It has anti‑angiogenic activity and is a valuable research tool in studies of tissue repair, wound healing, and vascularization. |
| Enzyme Assay |
Non‑cellular binding assays for LCKLSL hydrochloride involve measuring its ability to inhibit the binding of tPA to AnxA2. These assays can be performed using ELISA‑based competition assays where the peptide is incubated with recombinant AnxA2 and labeled tPA. The inhibition of binding is quantified, and IC50 values are determined from dose‑response curves.
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| Cell Assay |
In vitro cellular assays for LCKLSL hydrochloride are performed using various cell types to assess its effects on AnxA2‑mediated processes. Cells are treated with the peptide, and the inhibition of tPA binding to AnxA2 is confirmed. Plasmin generation is measured using chromogenic substrates. Anti‑angiogenic activity is assessed using endothelial cell tube formation assays.
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| Animal Protocol |
In vivo animal experiments for LCKLSL hydrochloride are conducted in mouse models of EAE to assess its effects on disease development. The peptide has also been studied in the mouse Matrigel plug assay and the chicken chorioallantoic membrane assay to assess anti‑angiogenic activity. Endpoints include disease severity, angiogenesis, and assessment of AnxA2 inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for LCKLSL hydrochloride are not extensively detailed in available sources. The peptide has a sequence of Leu‑Cys‑Lys‑Leu‑Ser‑Leu. The hydrochloride salt enhances solubility and stability. As a peptide, its PK would be influenced by factors such as proteolytic degradation and clearance. It is typically administered via injection for in vivo studies.
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| Toxicity/Toxicokinetics |
Toxicological data for LCKLSL hydrochloride are not extensively detailed in available sources. As a research peptide, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption. Standard safety precautions for handling peptides should be followed.
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| References | |
| Additional Infomation |
LCKLSL hydrochloride is an N‑terminal hexapeptide and a competitive annexin A2 (AnxA2) inhibitor that potently inhibits the binding of tPA to AnxA2. It inhibits plasmin generation and has anti‑angiogenic activity. It inhibits EAE development in mice and is a valuable research tool in studies of tissue repair, wound healing, and vascularization. It is not approved for clinical use.
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| Molecular Formula |
C30H58CLN7O8S
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|---|---|
| Molecular Weight |
712.34
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| Related CAS # |
LCKLSL;533902-29-3
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~25 mg/mL (~35.10 mM)
H2O :~10 mg/mL (~14.04 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 8.33 mg/mL (11.69 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4038 mL | 7.0191 mL | 14.0382 mL | |
| 5 mM | 0.2808 mL | 1.4038 mL | 2.8076 mL | |
| 10 mM | 0.1404 mL | 0.7019 mL | 1.4038 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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