ChemicalBook CAS DataBase List 1115270-63-7

1115270-63-7

Name	IAXO-102
CAS	1115270-63-7
Molecular Formula	C35H71NO5
MDL Number	MFCD31813901
Molecular Weight	585.94
MOL File	1115270-63-7.mol

Chemical Properties

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

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319-H335
Precautionary statements	P261-P305+P351+P338

Hazard Information

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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