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

Product Name
2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-
CAS No.
6318-41-8
Chemical Name
2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-
Synonyms
PI 3-Kγ Inhibitor VII;PI 3-Kγ Inhibitor VII;AS-041164, 10 mM in DMSO;AS-041164, PI3K gamma inhibitor;PI 3-Kγ Inhibitor VII - CAS 6318-41-8 - Calbiochem;2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-;5-(Benzo[d][1,3]dioxol-5-ylmethylene)thiazolidine-2,4-dione;Inhibitor,PI3Kγ,inhibit,Phosphoinositide 3-kinase,AS 041164,AS-041164,anti-inflammatory,neutrophil,recruitment,AS041164,RANTES,PI3K
CBNumber
CB13232856
Molecular Formula
C11H7NO4S
Formula Weight
249.24
MOL File
6318-41-8.mol
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2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Property

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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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
528114
Product name
PI 3-Kγ Inhibitor VII - CAS 6318-41-8 - Calbiochem
Packaging
5mg
Price
$238
Updated
2023/01/07
Cayman Chemical
Product number
13622
Product name
AS-041164
Packaging
10mg
Price
$92
Updated
2024/03/01
Cayman Chemical
Product number
13622
Product name
AS-041164
Packaging
50mg
Price
$346
Updated
2024/03/01
Cayman Chemical
Product number
13622
Product name
AS-041164
Packaging
5mg
Price
$72
Updated
2024/03/01
Cayman Chemical
Product number
13622
Product name
AS-041164
Packaging
25mg
Price
$207
Updated
2024/03/01
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2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Chemical Properties,Usage,Production

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] CHIARA FERRANDI. Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment.[J]. Journal of Pharmacology and Experimental Therapeutics, 2007, 322 3: 923-930. DOI:10.1124/jpet.107.123026

2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- Preparation Products And Raw materials

Raw materials

Preparation Products

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

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6318-41-8, 2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-Related Search:

LY 294002 Hydrochloride Oxaprozin GSK J1 Amlexanox ROLIPRAM 3-METHYLADENINE WORTMANNIN PI3-Kinase α Inhibitor 2

  • 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
  • 6318-41-8