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AS-041164

Names

[ CAS No. ]:
6318-41-8

[ Name ]:
AS-041164

[Synonym ]:
2,5-Thiazolidinedione, 4-(1,3-benzodioxol-5-ylmethylene)-, (4E)-
5-Piperonyliden-2,4-thiazolidindion
(4E)-4-(1,3-Benzodioxol-5-ylmethylene)-1,3-thiazolidine-2,5-dione
5-piperonylidene-thiazolidine-2,4-dione
5-Piperonyliden-thiazolidin-2,4-dion

Biological Activity

[Description]:

AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects[1].

[Related Catalog]:

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K
Research Areas >> Inflammation/Immunology

[Target]

PI3Kγ:70 nM (IC50)

PI3Kα:240 nM (IC50)

PI3Kβ:1.4 μM (IC50)

PI3Kδ:1.7 μM (IC50)


[In Vivo]

AS-041164 (10-100 mg/kg; oral administration; once) treatment results in the reduction of inflammatory swelling in the model of carrageenan-induced paw edema[1]. AS-041164 (3-100 mg/kg p.o.) treatment dose-dependently decreases r-h regulated on activation normal T cell expressed and secreted (RANTES)-induced neutrophil recruitment in mice. The ED50 value for AS-041164 is 27.35 mg/kg. AS-041164 blocks RANTES-induced chemotaxis and reduces the level of AKT phosphorylation[1]. Animal Model: Male Wistar rats (100-150 g) injected with carrageenan[1] Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: Oral administration; once Result: Induced a significant reduction of paw thickness.

[References]

[1]. Chiara Ferrandi, et al. Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment. J Pharmacol Exp Ther. 2007 Sep;322(3):923-30.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C11H7NO4S

[ Molecular Weight ]:
249.243

[ Exact Mass ]:
249.009583

[ PSA ]:
89.93000

[ LogP ]:
2.46

[ Index of Refraction ]:
1.731

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds