Basic information Safety Supplier Related

2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-

Basic information Safety Supplier Related

2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Basic information

Product Name:
2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-
Synonyms:
  • 2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-
  • PI 3-Kγ Inhibitor VII - CAS 6318-41-8 - Calbiochem
  • Inhibitor,PI3Kγ,inhibit,Phosphoinositide 3-kinase,AS 041164,AS-041164,anti-inflammatory,neutrophil,recruitment,AS041164,RANTES,PI3K
  • 5-(Benzo[d][1,3]dioxol-5-ylmethylene)thiazolidine-2,4-dione
  • AS-041164, PI3K gamma inhibitor
  • AS-041164, 10 mM in DMSO
  • PI 3-Kγ Inhibitor VII
  • PI 3-Kγ Inhibitor VII
CAS:
6318-41-8
MF:
C11H7NO4S
MW:
249.24
Mol File:
6318-41-8.mol
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2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Chemical Properties

Density 
1.595±0.06 g/cm3(Predicted)
storage temp. 
+2C to +8C
solubility 
Soluble in DMSO (up to 25 mg/ml).
form 
Yellow solid
pka
7.13±0.20(Predicted)
color 
Yellow
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
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2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Usage And Synthesis

Description

The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism. AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM). When tested at 1.0 μM, it shows little or no activity against 38 other common kinases. When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES.

Uses

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].

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.

IC 50

PI3Kγ: 70 nM (IC50); PI3Kα: 240 nM (IC50); PI3Kβ: 1.4 μM (IC50); PI3Kδ: 1.7 μM (IC50)

References

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

2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-Supplier

BOC Sciences
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1-631-485-4226; 16314854226
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info@bocsci.com
Shanghai EFE Biological Technology Co., Ltd.
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021-65675885 18964387627
Email
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Shanghai YuanYe Biotechnology Co., Ltd.
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021-61312847; 18021002903
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Tianjin Kailiqi Biotechnology Co., Ltd.
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15076683720
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klq@cw-bio.com
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
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2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-(6318-41-8)Related Product Information