AS1949490

Catalog No.E0400 Batch:E040001

Technical Data

Formula	C₂₀H₁₈ClNO₂S
Molecular Weight	371.88	CAS No.	1203680-76-5
Solubility (25°C)*	In vitro	DMSO	74 mg/mL (198.98 mM)
		Ethanol	37 mg/mL (99.49 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

AS1949490, a competitive inhibitor of 5'-lipid phosphatase SHIP2 with IC50 values of 0.62 µM and 0.34 µM for human (Ki value is 0.44 µM) and mouse respectively, promotes protein kinase C-dependent stabilization of brain-derived neurotrophic factor mRNA in cultured cortical neurons.

Targets

Human SHIP2 ^[1]	Human SHIP2 ^[1]	Mouse SHIP2 ^[1]
0.44 μM(Ki)	0.62 μM	0.62 μM

In vitro

AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake in L6 myotubes. In FAO hepatocytes, AS1949490 suppresses gluconeogenesis.^[1]

In vivo

Acute administration of AS1949490 inhibites the expression of gluconeogenic genes in the livers of normal mice. Chronic treatment of diabetic db/db mice with AS1949490 significantly loared the plasma glucose level and improved glucose intolerance.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines L6 myotubes, FAO hepatocytes Concentrations 1-16 µM Incubation Time 15 min, 24 h, 48 h Method L6 myotubes are incubated for 15 min both with and without AS1949490 treatment before being stimulated with insulin at indicated concentration and 1 nM or fetal bovine serum at indicated concentrations for 10 min. Protein lysates from L6 myotubes are immunoblotted with anti-phosphorylated Akt antibody or anti-Akt antibody. FAO cells are treated with AS19494940 and insulin for 24 h. The glucose concentration in the medium is measured after incubation for 6 h in gluconeogenesis buffer.

Cell Assay:^{^[1]}

Cell lines
L6 myotubes, FAO hepatocytes
Concentrations
1-16 µM
Incubation Time
15 min, 24 h, 48 h
Method
L6 myotubes are incubated for 15 min both with and without AS1949490 treatment before being stimulated with insulin at indicated concentration and 1 nM or fetal bovine serum at indicated concentrations for 10 min. Protein lysates from L6 myotubes are immunoblotted with anti-phosphorylated Akt antibody or anti-Akt antibody. FAO cells are treated with AS19494940 and insulin for 24 h. The glucose concentration in the medium is measured after incubation for 6 h in gluconeogenesis buffer.

References

[1] Suwa A, et al. Br J Pharmacol. 2009 Oct;158(3):879-87.

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