IAXO-102
IAXO-102 Basic information
- Product Name:
- IAXO-102
- Synonyms:
-
- IAXO-102
- α-D-Glucopyranoside, methyl 6-amino-6-deoxy-2,3-di-O-tetradecyl-
- Methyl 6-amino-6-deoxy-2,3-di-O-tetradecyl-α-D-glucopyranoside
- IAXO102,IAXO 102,Toll-like Receptor (TLR),Inhibitor,IAXO-102,inhibit
- IAXO-102 (CD14/TLR4 Antagonist) (synthetic)
- IAXO-102 ，S0002
- CAS:
- 1115270-63-7
- MF:
- C35H71NO5
- MW:
- 585.96
- Mol File:
- 1115270-63-7.mol
IAXO-102 Chemical Properties
- Boiling point:
- 650.2±55.0 °C(Predicted)
- Density
- 0.96±0.1 g/cm3(Predicted)
- storage temp.
- under inert gas (nitrogen or Argon) at 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
IAXO-102 Usage And Synthesis
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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