| Identification | Back Directory | [Name]
IAXO-102 | [CAS]
1115270-63-7 | [Synonyms]
IAXO-102
α-D-Glucopyranoside, methyl 6-amino-6-deoxy-2,3-di-O-tetradecyl- | [Molecular Formula]
C35H71NO5 | [MDL Number]
MFCD31813901 | [MOL File]
1115270-63-7.mol | [Molecular Weight]
585.94 |
| Chemical Properties | Back Directory | [Boiling point ]
650.2±55.0 °C(Predicted) | [density ]
0.96±0.1 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
Ethanol : 50 mg/mL (85.33 mM; Need ultrasonic)|DMSO : 5 mg/mL (8.53 mM; Need ultrasonic) | [form ]
A solid | [pka]
13.00±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development[1]. | [Biological Activity]
IAXO-102 is a TLR4 antagonist targeting the MD-2 and CD14 co-receptors,which inhibits MAPK and p65 NF-κB phosphorylation and downregulates the expression of TLR4-dependent pro-inflammatory proteins. It inhibits the development of experimental abdominal aortic aneurysm (AAA). | [in vitro]
IAXO-102 (1-10 μM, for 2 hours) inhibits MAPK and p65 NF-κB phosphorylation in human umbilical vein endothelial (HUVEC) cells.
IAXO-102 (10 μM, for 17 hours) suppresses LPS induced proinflammatory proteins MCP-1 and IL-8 production in HUVEC. Western Blot Analysis | Cell Line: | Human umbilical vein endothelial (HUVEC) cells | | Concentration: | 1-10 μM | | Incubation Time: | Pretreatment for 1 hour and then exposed to LPS (100 ng/mL) for additional 1 hour | | Result: | Significantly inhibited LPS- stimulated MAPK/p65nF-ΚB phosphorylation. | | [in vivo]
IAXO-102 (3 mg/kg/day, sc for 28 days) significantly retards Angiotensin II induced increase in aortic diameter in mice. | Animal Model: < /td> | Six-monthold ApoE ?/? /C57Bl6 | | Dosage: | 3 mg/kg/day | | Administration: | SC for 28 days | | Result: | Significantly retarded Angiotensin II -induced increase in aortic diameter. | | [target]
| Target | Value | TLR4
() | MAPK
() | NF-κB
() |
| [IC 50]
TLR4 | [References]
[1] Huggins C, et al. A novel small molecule TLR4 antagonist (IAXO-102) negatively regulates non-hematopoietic toll like receptor 4 signalling and inhibits aortic aneurysms development. Atherosclerosis. 2015 Oct;242(2):563-70. DOI:10.1016/j.atherosclerosis.2015.08.010 |
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