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BIO-11006 acetate

Cat No.:V77205 Purity: ≥98%
BIO-11006 acetate, an analog of MANS peptide, is a MARCKS (myristoylated alanine-rich C kinase substrate) inhibitor.
BIO-11006 acetate
BIO-11006 acetate Chemical Structure Product category: Peptides
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
5mg
10mg
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Product Description
BIO-11006 acetate, an analog of MANS peptide, is a MARCKS (myristoylated alanine-rich C kinase substrate) inhibitor.
BIO-11006 acetate is a peptide inhibitor of the Myristoylated Alanine-Rich C Kinase Substrate (MARCKS) protein, an analog of the MANS peptide. It is indicated for research on acute lung injury/acute respiratory distress syndrome (ALI/ARDS). The compound attenuates LPS-induced neutrophil influx into the lungs, NF-kappaB activation, and expression of proinflammatory cytokines KC and TNF-alpha, reversing disease progression in LPS-induced mouse lung injury models.
Biological Activity I Assay Protocols (From Reference)
Targets
Myristoylated alanine-rich C kinase substrate[1]
BIO-11006 acetate targets the MARCKS (Myristoylated Alanine-Rich C Kinase Substrate) protein, which is involved in various cellular processes including cell adhesion, migration, and secretion. MARCKS is a substrate for protein kinase C (PKC) and plays a role in the regulation of the actin cytoskeleton. By inhibiting MARCKS function, BIO-11006 modulates inflammatory responses in the lung, particularly neutrophil recruitment and cytokine production.
ln Vitro
In vitro, BIO-11006 is shown to inhibit MARCKS function, though specific cellular EC50 values are not detailed in available literature. The compound has been studied for its ability to reduce proinflammatory responses in lung epithelial cells and macrophages. It attenuates NF-kappaB activation and decreases expression of inflammatory mediators such as KC (IL-8 homolog) and TNF-alpha in response to lipopolysaccharide (LPS) stimulation.
ln Vivo
In mice given intratracheal injections of LPS, inhaled, aerosolized BIO-11006 acetate reverses the development of lung injury by attenuating LPS-induced neutrophil influx into the lung, activation of NF-κB, and production of the proinflammatory cytokines, KC and TNF-α [1].
In vivo, BIO-11006 acetate (inhaled, aerosolized formulation) attenuates LPS-induced neutrophil influx into the lung, activation of NF-kappaB, and expression of proinflammatory cytokines KC and TNF-alpha, thereby reversing the development of lung injury in mice instilled intratracheally with LPS. The compound demonstrates efficacy in reversing disease progression in this acute lung injury model, supporting its research application for ALI/ARDS.
Enzyme Assay
Binding assays for BIO-11006 focus on its interaction with the MARCKS protein. Typically, these studies employ surface plasmon resonance (SPR) or fluorescence polarization techniques to measure the binding affinity between the peptide and the MARCKS effector domain. Alternatively, competitive binding assays using labeled MARCKS peptides and the compound can be performed to determine IC50 or Kd values, confirming direct protein-peptide interaction.
Cell Assay
Cellular experiments for BIO-11006 utilize LPS-stimulated lung epithelial cells or macrophage cell lines such as RAW 264.7 or THP-1 cells. Cells are treated with varying concentrations of BIO-11006 for a defined period (e.g., 24-48 hours), then stimulated with LPS to induce inflammation. Endpoints include measurement of NF-kappaB activation by luciferase reporter assay or immunoblotting, quantification of proinflammatory cytokines (TNF-alpha, IL-6, KC) by ELISA in culture supernatants, and assessment of cell viability by MTT assay.
Animal Protocol
Animal studies for BIO-11006 are typically conducted in a mouse model of LPS-induced acute lung injury. Mice receive an intratracheal instillation of LPS to trigger lung inflammation. BIO-11006 acetate (inhalation or aerosolized) is administered either prophylactically or therapeutically. Endpoints include bronchoalveolar lavage fluid (BALF) analysis for neutrophil count and cytokine levels, lung histopathology for injury scoring, and Western blotting for NF-kappaB pathway activation markers.
ADME/Pharmacokinetics
A drug-specific pharmacokinetic (PK) properties of BIO-11006 are not listed in typical product literature. Since BIO-11006 is a peptide, its distribution and metabolic stability are likely to be evaluated via assays such as plasma stability testing and in vivo sampling, but PK parameters like bioavailability, half-life, and clearance are not readily available in general product descriptions and would be found in specialized pharmacology studies.
Toxicity/Toxicokinetics
Toxicological data for BIO-11006 are not extensively detailed in available product literature. The compound has been studied in mouse models of acute lung injury and has shown efficacy without reports of significant adverse effects in the published studies. Standard preclinical toxicology assessments including acute and repeated-dose toxicity would be required for therapeutic development. For research use, standard peptide handling precautions apply.
References

[1]. An Inhaled Inhibitor of Myristoylated Alanine-Rich C Kinase Substrate Reverses LPS-Induced Acute Lung Injury in Mice. Am J Respir Cell Mol Biol. 2016 Nov;55(5):617-622.

Additional Infomation
BIO-11006 acetate (CAS 901117-03-1) has the molecular formula C46H75N13O15 and a molecular weight of 1050.17. It is a peptide analog of the MANS peptide and functions as a MARCKS inhibitor. The compound is administered by inhalation or aerosolization in mouse models. It is indicated for research on acute lung injury/acute respiratory distress syndrome (ALI/ARDS). Clinical development status is not specified, but it is currently a research tool. It is for research use only and not for human therapy.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C48H79N13O17
Molecular Weight
1110.22
Appearance
White to off-white solid powder
HS Tariff Code
2934.99.9001
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, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O :~50 mg/mL (~45.04 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.25 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 (2.25 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (2.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly.


Solubility in Formulation 4: 20 mg/mL (18.01 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.9007 mL 4.5036 mL 9.0072 mL
5 mM 0.1801 mL 0.9007 mL 1.8014 mL
10 mM 0.0901 mL 0.4504 mL 0.9007 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.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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