| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
TLR4
Kdo2-Lipid A ammonium likely targets Toll-like receptor 4 (TLR4), the receptor for lipopolysaccharide (LPS). Lipid A is the bioactive component of LPS that activates TLR4, triggering inflammatory responses. Kdo2-Lipid A is a well-defined chemotype of lipid A that is used as a standard for studying TLR4 signaling and endotoxin biology. The ammonium salt form may enhance solubility for research applications. |
|---|---|
| ln Vitro |
In adult rat spinal astrocyte cell cultures, Kdo2-Lipid A (1 µM) promotes the secretion of both PGE2 and TNF[1].
In vitro data for Kdo2-Lipid A ammonium is not extensively reported in publicly available sources. As a lipid A derivative, it is expected to activate TLR4 signaling in immune cells, leading to the production of pro-inflammatory cytokines such as TNF-α, IL-6, and IL-1β. It may be used as a reference standard in assays measuring TLR4 activation or endotoxin neutralization. However, specific activity data for this compound has not been detailed in the available literature. |
| ln Vivo |
In rats, KDO2-Lipid A (it) stimulates toll-like receptor 4 (TLR4)[1].
In vivo data for Kdo2-Lipid A ammonium is not extensively reported in publicly available sources. As a lipid A derivative, it would be expected to induce inflammatory responses in animal models, similar to LPS. It may be used in studies of sepsis, endotoxemia, or immune activation. However, specific published in vivo efficacy studies for Kdo2-Lipid A ammonium are not detailed in the current literature. |
| Enzyme Assay |
The in vitro TLR4 activation assay for Kdo2-Lipid A ammonium would typically use TLR4-expressing cells such as macrophages or HEK293 cells transfected with TLR4/MD2. Cells are treated with varying concentrations of the compound, and TLR4 activation is measured by quantifying NF-κB activation, cytokine production (e.g., TNF-α, IL-6), or reporter gene expression. The compound may be used as a positive control for TLR4 activation.
|
| Cell Assay |
RT-PCR[1]
Cell Types: TNF and PGE2 Tested Concentrations: 1 µM Incubation Duration: Experimental Results: Amounts of protein (mg) is 6.2 ± 0.6 ng/mL and 1.4 ± 0.3 ng/mL for TNF and PGE2. Cellular assays for Kdo2-Lipid A ammonium are conducted in immune cells such as macrophages or dendritic cells. Cells are treated with varying concentrations of the compound, and inflammatory responses are assessed by measuring cytokine production using ELISA or qPCR. TLR4 signaling is evaluated by Western blotting for phosphorylated signaling proteins such as NF-κB and MAP kinases. Cell viability is assessed using standard assays. |
| Animal Protocol |
Animal/Disease Models: Rats (Male Holzman SD (Sprague-Dawley), 300–400 g) [1]
Doses: 0.1 to 10 µg Route of Administration: IT; 0.1-10 µg; prior and 15, 30, 60, 90 and 120 min after injection of Kdo2-Lipid A. Experimental Results: Intrathecal injection of 1 µg Kdo2-Lipid A induces allodynia, and the animals appeared to be sick after it injection of Kdo2-Lipid A. In vivo studies for Kdo2-Lipid A ammonium would typically involve mouse models of endotoxemia or sepsis. The compound would be administered via intraperitoneal or intravenous injection, and inflammatory responses would be assessed by measuring cytokine levels in serum, body temperature, and survival. However, specific published in vivo protocols for Kdo2-Lipid A ammonium are not available in the current literature. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Kdo2-Lipid A ammonium is not extensively reported in publicly available sources. As a lipid A derivative, it is expected to have limited oral bioavailability and is typically administered via injection for in vivo studies. Detailed PK parameters such as half-life and bioavailability are not available in the current literature for this research compound.
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| Toxicity/Toxicokinetics |
Toxicity data for Kdo2-Lipid A ammonium is limited in publicly available sources. As a lipid A derivative, it is expected to be toxic at high doses due to its potent inflammatory activity. As with all research compounds, Kdo2-Lipid A ammonium is intended for research use only and not for human therapeutic applications. Appropriate safety precautions should be taken when handling this compound due to its endotoxic activity.
|
| References | |
| Additional Infomation |
Kdo2-Lipid A ammonium (CAS 1246298-62-3) is a research compound that is likely a derivative of lipid A, the endotoxic component of lipopolysaccharide (LPS). It is used in immunology and inflammation research to study TLR4 signaling and endotoxin biology. The ammonium salt form may enhance solubility for research applications. Further information on this compound would require access to specialized chemical databases or the original literature.
|
| Molecular Formula |
C110H214N6O39P2
|
|---|---|
| Molecular Weight |
2306.84
|
| Exact Mass |
2325.263
|
| CAS # |
1246298-62-3
|
| PubChem CID |
163358722
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
19
|
| Hydrogen Bond Acceptor Count |
40
|
| Rotatable Bond Count |
98
|
| Heavy Atom Count |
154
|
| Complexity |
3760
|
| Defined Atom Stereocenter Count |
24
|
| SMILES |
CCCCCCCCCCCCCC(=O)O[C@H](CCCCCCCCCCC)CC(=O)O[C@@H]1[C@H]([C@@H](O[C@@H]([C@H]1OP(=O)(O)O)CO[C@@]2(C[C@H]([C@@H]([C@H](O2)[C@@H](CO)O)O)O[C@@]3(C[C@H]([C@@H]([C@H](O3)[C@@H](CO)O)O)O)C(=O)O)C(=O)O)OC[C@@H]4[C@H]([C@@H]([C@H]([C@H](O4)OP(=O)(O)O)NC(=O)C[C@@H](CCCCCCCCCCC)O)OC(=O)C[C@@H](CCCCCCCCCCC)O)O)NC(=O)C[C@@H](CCCCCCCCCCC)OC(=O)CCCCCCCCCCC.N
|
| InChi Key |
LQKZRFADNCODFM-UIHQQFNTSA-N
|
| InChi Code |
InChI=1S/C110H202N2O39P2.H3N/c1-7-13-19-25-31-37-38-44-50-56-62-68-92(123)142-82(66-60-54-48-42-35-29-23-17-11-5)72-94(125)146-104-96(112-90(121)71-81(65-59-53-47-41-34-28-22-16-10-4)141-91(122)67-61-55-49-43-36-30-24-18-12-6)105(144-88(102(104)150-152(133,134)135)78-140-109(107(129)130)74-86(98(127)101(148-109)85(119)76-114)147-110(108(131)132)73-83(117)97(126)100(149-110)84(118)75-113)139-77-87-99(128)103(145-93(124)70-80(116)64-58-52-46-40-33-27-21-15-9-3)95(106(143-87)151-153(136,137)138)111-89(120)69-79(115)63-57-51-45-39-32-26-20-14-8-2;/h79-88,95-106,113-119,126-128H,7-78H2,1-6H3,(H,111,120)(H,112,121)(H,129,130)(H,131,132)(H2,133,134,135)(H2,136,137,138);1H3/t79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,95-,96-,97+,98+,99-,100-,101-,102-,103-,104-,105-,106-,109-,110-;/m1./s1
|
| Chemical Name |
azane;(2R,4R,5S,6R)-2-[(2R,4R,5S,6R)-2-carboxy-6-[(1R)-1,2-dihydroxyethyl]-2-[[(2R,3S,4R,5R,6R)-5-[[(3R)-3-dodecanoyloxytetradecanoyl]amino]-6-[[(2R,3S,4R,5R,6R)-3-hydroxy-5-[[(3R)-3-hydroxytetradecanoyl]amino]-4-[(3R)-3-hydroxytetradecanoyl]oxy-6-phosphonooxyoxan-2-yl]methoxy]-3-phosphonooxy-4-[(3R)-3-tetradecanoyloxytetradecanoyl]oxyoxan-2-yl]methoxy]-5-hydroxyoxan-4-yl]oxy-6-[(1R)-1,2-dihydroxyethyl]-4,5-dihydroxyoxane-2-carboxylic acid
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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, 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 (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 | 0.4335 mL | 2.1675 mL | 4.3349 mL | |
| 5 mM | 0.0867 mL | 0.4335 mL | 0.8670 mL | |
| 10 mM | 0.0433 mL | 0.2167 mL | 0.4335 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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