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| 10mg |
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| Other Sizes |
| ln Vitro |
Boc-Phe-Leu-Phe-Leu-Phe (0-50 μg/mL) inhibited HUVEC spheroid budding induced by PDR vitreous body in three-dimensional fibrin gel [1]. Boc-Phe-Leu-Phe-Leu-Phe (0-120 μM, 24 h) inhibited VEGF-mediated HUVEC spheroid budding in a dose-dependent manner [2]. Boc-Phe-Leu-Phe-Leu-Phe (100 ng/mL, 24 h) inhibited the ability of Ac2-26 to reduce LPS-induced expression of TGF-β1, IL-1β and IL-6 in RAW264.7 cells [4]. Boc-Phe-Leu-Phe-Leu-Phe (100 ng/mL, 24 h) blocked the inhibitory effect of Ac2-26 on the expression of α-SMA, type I collagen, CTGF and β-catenin in LPS-induced hepatic stellate cells (HSCs) [4]. Boc-Phe-Leu-Phe-Leu-Phe (10 µM) blocked the inhibitory effect of Ac2-26 on the increase of AnxA1 protein expression, the increase of phosphorylated NF-κB p65 level, the degradation of IκB-α and the production of IL-8 in A549 cells [5].
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| ln Vivo |
Boc-Phe-Leu-Phe-Leu-Phe (1 mg/kg, intraperitoneal injection, twice a week for 4–8 weeks) reversed the anti-inflammatory and anti-fibrotic effects of Ac2-26 on CCl4-induced liver fibrosis in wild-type mice and AnxA1 knockout mice [4]. Boc-Phe-Leu-Phe-Leu-Phe (50 µg per rat, intraperitoneal injection 30 minutes before surgery, single dose) reversed the protective effect of Ac2-26 in rats with ischemia-reperfusion-induced acute lung injury [5].
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| Cell Assay |
Real-time quantitative PCR[4]
Cell Types: LPS ( ) induced RAW264.7 cells Tested Concentrations: 100 ng/mL Incubation Duration: 24 hours Experimental Results: The expression of TGF-β1, IL-1β and IL-6 was reduced. Western Blot analysis [4] Cell Types: LPS ( ) induced RAW264.7 cells Tested Concentrations: 100 ng/mL Incubation Duration: 24 hours Experimental Results: α-SMA, type I collagen, CTGF and β-catenin expression were decreased. |
| Animal Protocol |
Animal/Disease Models:6-8 week old C57BL/6 wild-type mice and C57BL/6JGpt Anxa1-KO mice (18-25 g weight) were injected intraperitoneally twice a week with 20% CCl4 (500 mL) to induce liver fibrosis [4]
... The anti-inflammatory and anti-fibrotic effects of Ac2-26 were reversed, and the degree of liver damage and fibrosis was similar to that in the CCl4-induced model group that did not receive Ac2-26 treatment. Animal/Disease Models:Sprague-Dawley rats (male, 350±20 g) were used to establish an in vitro perfusion lung model. Ischemia was induced by stopping ventilation and perfusion for 40 minutes, followed by reperfusion for 60 minutes to induce ischemia-reperfusion lung injury [5]. Doses: 50 µg per rat. Route of Administration: Single dose administered intraperitoneally 30 minutes before surgery. Experimental Results: Ac2-26 was eliminated from its protective effect on ischemia-reperfusion induced acute lung injury in Sprague-Dawley rats, leading to increased pulmonary edema, increased pulmonary artery pressure, and increased protein concentration in bronchoalveolar lavage fluid. Increased neutrophil infiltration and elevated levels of pro-inflammatory cytokines (CINC-1, TNF-α) were observed in bronchoalveolar lavage fluid. Oxidative stress (increased protein carbonyl content and MDA levels) and apoptosis (increased caspase-3-labeled activated cells and decreased Bcl-2 expression) were also observed in lung tissue. Lung tissue damage was aggravated, lung injury scores increased, and alveolar wall tight junction proteins (claudin-3, occludin, ZO-1) were disrupted. Ac2-26 reversed the inhibitory effect of NF-κB and MAPK pathway activation. |
| References |
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| Molecular Formula |
C44H59N5O8
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|---|---|
| Molecular Weight |
785.97
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| CAS # |
73572-58-4
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| Related CAS # |
Boc-dPhe-Leu-dPhe-Leu-Phe; BOC-FlFlF
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| Sequence |
{Boc}-Phe-Leu-Phe-Leu-Phe{Boc}-FLFLF
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| SequenceShortening |
{Boc}-FLFLF
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| Appearance |
White to off-white solid
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| SMILES |
O=C([C@H](CC(C)C)NC([C@H](CC1C=CC=CC=1)NC(=O)OC(C)(C)C)=O)N[C@H](C(N[C@H](C(N[C@H](C(=O)O)CC1C=CC=CC=1)=O)CC(C)C)=O)CC1C=CC=CC=1
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| Synonyms |
L-BOC2
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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: 请将本产品存放在密封保护的环境中，避免受潮。 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2723 mL | 6.3616 mL | 12.7231 mL | |
| 5 mM | 0.2545 mL | 1.2723 mL | 2.5446 mL | |
| 10 mM | 0.1272 mL | 0.6362 mL | 1.2723 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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