| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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IAXO-102 is a novel and potent TLR4 antagonist with anti-inflammatory effects. It inhibits MAPK and p65 NF-kB phosphorylation involved in down regulation of the expression of TLR4 and TLR4 dependent proinflammatory proteins.
| ln Vitro |
IAXO-102 (1–10 μM) inhibits p65 NF-κB and MAPK phosphorylation for two hours in human vascular endothelial (HUVEC) cells [1]. IAXO-102 (10 μM) inhibits HUVEC for 17 hours.
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|---|---|
| ln Vivo |
The aortic dilatation caused by angiotensin II is markedly postponed by IAXO-102 (3 mg/kg/day, administered subcutaneously for 28 days) [1].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Human Umbilical Vein Endothelial (HUVEC) Cells Tested Concentrations: 1-10 µM Incubation Duration: 1 hour pretreatment, then 1] LPS Induced production of the pro-inflammatory proteins MCP-1 and IL-8. Then exposed to LPS (100 ng/mL) for 1 hour. Experimental Results: Significant inhibition of LPS-stimulated MAPK/p65nF-KB phosphorylation. |
| Animal Protocol |
Animal/Disease Models: Six-month-old ApoE−/−/C57Bl6[1]
Doses: 3 mg/kg/day Route of Administration: SC 28 days Experimental Results: Dramatically delayed angiotensin II-induced increase in aortic diameter. |
| References |
| Molecular Formula |
C35H71NO5
|
|---|---|
| Molecular Weight |
585.941951990128
|
| Exact Mass |
585.533
|
| CAS # |
1115270-63-7
|
| PubChem CID |
25222900
|
| Appearance |
White to off-white solid powder
|
| LogP |
12.1
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
30
|
| Heavy Atom Count |
41
|
| Complexity |
537
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
O1[C@@H]([C@@H]([C@H]([C@@H]([C@H]1CN)O)OCCCCCCCCCCCCCC)OCCCCCCCCCCCCCC)OC
|
| InChi Key |
DJVFNDPRLMVKKO-KJQSSVQNSA-N
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| InChi Code |
InChI=1S/C35H71NO5/c1-4-6-8-10-12-14-16-18-20-22-24-26-28-39-33-32(37)31(30-36)41-35(38-3)34(33)40-29-27-25-23-21-19-17-15-13-11-9-7-5-2/h31-35,37H,4-30,36H2,1-3H3/t31-,32-,33+,34-,35+/m1/s1
|
| Chemical Name |
(2R,3R,4S,5R,6S)-2-(aminomethyl)-6-methoxy-4,5-di(tetradecoxy)oxan-3-ol
|
| 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 |
| 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) |
Ethanol : ~50 mg/mL (~85.33 mM)
DMSO : ~5 mg/mL (~8.53 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.42 mM) (saturation unknown) in 10% EtOH + 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 8.3 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (1.42 mM) (saturation unknown) in 10% EtOH + 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 8.3 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7067 mL | 8.5333 mL | 17.0666 mL | |
| 5 mM | 0.3413 mL | 1.7067 mL | 3.4133 mL | |
| 10 mM | 0.1707 mL | 0.8533 mL | 1.7067 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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