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| Targets |
Toll-like receptor 2 (TLR2). Lipoteichoic acid is a key component of the cell wall in Gram-positive bacteria that specifically binds to Toll-like receptor 2 (TLR2). This binding triggers NF-κB signaling and the subsequent release of pro-inflammatory cytokines such as TNF-α and IL-6. LTA also activates the complement system by inducing C3 and inhibiting CD55. As a PAMP, LTA is recognized by the innate immune system as a signal of bacterial infection.
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| ln Vitro |
Lipoteichoic acid activates the complement system by inducing C3 and inhibiting CD55, and reduces fat deposition via the IGF-1 pathway. As a TLR2 agonist, LTA stimulates immune cells to produce pro-inflammatory cytokines including TNF-α and IL-6. The compound's ability to activate innate immune responses through TLR2 and complement pathways makes it a valuable tool for studying Gram-positive bacterial infections and host immune responses.
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| ln Vivo |
In vivo, Lipoteichoic acid is used as a potent inflammatory stimulus in animal models of sepsis and inflammation. It induces systemic inflammatory responses through TLR2 activation and complement system engagement. LTA is commonly used to model Gram-positive bacterial infections and to study host-pathogen interactions. The compound's ability to trigger NF-κB signaling and cytokine release in vivo makes it a valuable tool for studying innate immune responses and inflammatory disease mechanisms.
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| Enzyme Assay |
Receptor binding assays are used to characterize the interaction of Lipoteichoic acid with TLR2. ELISA-based or surface plasmon resonance assays are performed with recombinant human TLR2 protein, and increasing concentrations of LTA are added to determine binding affinity. Competition assays with known TLR2 ligands can confirm specific binding. Additionally, LTA binding to CD55 and its effects on complement activation can be assessed in biochemical assays.
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| Cell Assay |
Cellular assays using TLR2-expressing immune cells (e.g., macrophages, dendritic cells, or HEK293 cells transfected with TLR2) are employed to evaluate the immunostimulatory activity of Lipoteichoic acid. Cells are stimulated with increasing concentrations of LTA, and activation of NF-κB signaling is measured by reporter gene assays or by detecting phosphorylated signaling proteins. Cytokine production (TNF-α, IL-6, IL-1β) is measured by ELISA or multiplex assays to quantify the inflammatory response.
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| Animal Protocol |
In vivo efficacy of Lipoteichoic acid is evaluated in murine models of sepsis and inflammation. LTA is typically administered via intraperitoneal or intravenous injection at doses ranging from 1-50 mg/kg. Efficacy endpoints include measurement of pro-inflammatory cytokine levels in serum, immune cell infiltration into tissues, and survival rates. LTA-induced inflammation models are used to test the efficacy of anti-inflammatory compounds and to study the pathophysiology of Gram-positive bacterial infections.
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| ADME/Pharmacokinetics |
As a bacterial cell wall component with molecular weight of 775.0 g/mol, Lipoteichoic acid is administered via parenteral routes (intraperitoneal or intravenous) in animal studies. The compound is a polymer of glycerol phosphate units with a lipid anchor, which contributes to its amphipathic properties. Pharmacokinetic properties are characteristic of bacterial PAMPs, with rapid clearance and distribution to immune organs. LTA is not intended for human therapeutic use and is for research purposes only.
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| Toxicity/Toxicokinetics |
No specific toxicity data has been reported for Lipoteichoic acid. As a bacterial cell wall component, LTA is used as a pro-inflammatory stimulus and is not intended for human therapeutic use. At high doses, LTA can induce severe systemic inflammation and septic shock-like symptoms in animal models, which is a manifestation of its pharmacological activity rather than off-target toxicity. Standard safety precautions should be observed when handling this research reagent.
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| References | |
| Additional Infomation |
Lipotechiic acid (LTA) has been reported to exist in Streptococcus pyogenes, and relevant data are available. LTA is a biologically active lipopolysaccharide component of the cell wall of Gram-negative bacteria. LTA can bind non-specifically to the cell surface through interaction with phospholipids, or specifically to the cell surface through interaction with CD14 or Toll-like receptors (TLRs), subsequently being endocytosed. Binding to TLR2 can activate the NF-κB pathway, the mitogen-activated protein kinase (MAPK) signaling pathway, and phosphatidylinositol 3-kinase (PI3K) activity. This may lead to increased expression of pro-inflammatory cytokines and pro-apoptotic and anti-apoptotic genes, and may stimulate the expression of the immunosuppressive receptor programmed cell death protein 1 (PD-1; PDCD1; CD279). Increased PD-1 expression promotes its binding to ligands programmed death receptor 1 ligand 1 (PD-L1) or 2 (PD-L2), thereby stimulating the production of the anti-inflammatory cytokine interleukin-10 (IL-10) and leading to suppression of CD4-positive T cell proliferation and activity. Furthermore, LTA may induce cancer cell proliferation in some susceptible tumor cells while inhibiting the proliferation of other cancer cells. Finally, LTA levels in patient samples may be associated with inflammatory damage during acute bacterial infection.
Lipoteichoic acid (LTA) is a major amphipathic constituent of the cell wall of Gram-positive bacteria. It consists of a polyglycerol phosphate chain covalently attached to a lipid anchor. LTA serves as a PAMP that specifically binds to TLR2 and activates NF-κB signaling. It also activates the complement system by inducing C3 and inhibiting CD55. LTA is an indispensable reagent in sepsis modeling, adjuvant research, and host-pathogen interaction studies. CAS: 56411-57-5; molecular formula: C39H70N2O13; molecular weight: 775.0 g/mol. |
| Molecular Formula |
C39H70N2O13
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| Molecular Weight |
774.978713512421
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| Exact Mass |
774.487
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| CAS # |
56411-57-5
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| PubChem CID |
137349712
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| Appearance |
White to off-white solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
29
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| Heavy Atom Count |
54
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
11
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| SMILES |
O(C1C(C(C(C(C)O1)N)O)NC(C)=O)C1C(C(OCC(COC(CCCCCC)=O)OC(CCCCCC=CCCCCCCC)=O)OC(CO)C1O)O
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| InChi Key |
PANDRCFROUDETH-YLSOAJEOSA-N
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| InChi Code |
InChI=1S/C39H70N2O13/c1-5-7-9-11-12-13-14-15-16-17-18-20-22-31(45)52-28(24-49-30(44)21-19-10-8-6-2)25-50-39-36(48)37(34(46)29(23-42)53-39)54-38-33(41-27(4)43)35(47)32(40)26(3)51-38/h14-15,26,28-29,32-39,42,46-48H,5-13,16-25,40H2,1-4H3,(H,41,43)/b15-14+/t26-,28-,29-,32+,33-,34-,35+,36-,37+,38+,39+/m1/s1
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| Chemical Name |
[(2S)-1-[(2S,3R,4S,5R,6R)-4-[(2S,3R,4S,5R,6R)-3-acetamido-5-amino-4-hydroxy-6-methyloxan-2-yl]oxy-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-3-heptanoyloxypropan-2-yl] (E)-pentadec-7-enoate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 100 mg/mL
H2O: 10 mg/mL |
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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 | 1.2904 mL | 6.4518 mL | 12.9036 mL | |
| 5 mM | 0.2581 mL | 1.2904 mL | 2.5807 mL | |
| 10 mM | 0.1290 mL | 0.6452 mL | 1.2904 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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