1. AS1949490

AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50, and >50 µM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes.

For research use only. We do not sell to patients.

AS1949490 Chemical Structure

AS1949490 Chemical Structure

CAS No. : 1203680-76-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 100 In-stock
10 mg USD 160 In-stock
25 mg USD 320 In-stock
50 mg USD 512 In-stock
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Description

AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC50 values of 0.34, 0.62, 13, >50, >50, and >50 µM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes[1][2].

IC50 & Target

IC50: 0.34 nM (Mouse SHIP2), 0.62 nM (Human SHIP2), 13 nM (Human SHIP1), >50 nM (Human PTEN), >50 nM (Human synaptojanin), and >50 µM (Human myotubularin)[1].

In Vitro

AS1949490 (0-16 μM; 15 min; L6 myotubes) increases insulin-induced phosphorylation of Akt[1].
AS1949490 (0-10 μM; 48 h) activates glucose metabolism and stimulates glucose uptake activity in L6 myotubes[1].
AS1949490 (0-10 μM; 24 h; L6 myotubes) decreases the level of insulin-induced gluconeogenesis[1].
AS1949490 (10 μM; 48 h) activates glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: L6 myotubes
Concentration: 0, 4, 8, and 16 µM; 1 nM (insulin)
Incubation Time: 15 minutes
Result: Increased insulin-induced phosphorylation of Akt in a dose-dependent manner.

Western Blot Analysis[2]

Cell Line: L6 myotubes
Concentration: 10 µM
Incubation Time: 48 hours
Result: Increased GLUT1 but not GLUT4 mRNA expression in L6 myotubes.
In Vivo

AS1949490 (300 mg/kg; p.o.; twice daily, for 7 or 10 d) decreases plasma glucose and activates intracellular insulin signalling in diabetic mice[1]. AS1949490 (300 mg/kg; p.o.; once, for 8 h; male ICR mice) suppresses gluconeogenesis and the expression of related genes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/KsJ Jcl-dbm mice and db/+db mice[1]
Dosage: 300 mg/kg
Administration: Oral administration; twice daily, for 7 or 10 days
Result: Decreased plasma glucose (23% reduction, relative to vehicle).
Reduced fasting blood glucose (37% reduction, relative to vehicle) and the area under the blood glucose concentration time curve (AUC).
Increased the phosphorylation of GSK3β in the liver without changing the overall levels of GSK3β protein.
Animal Model: Male ICR mice (6 weeks of age)[1]
Dosage: 300 mg/kg
Administration: Oral administration; once, for 8 hours
Result: Reduced an approximately 50% of both PEPCK and G6Pase mRNA levels.
Molecular Weight

371.88

Formula

C20H18ClNO2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(OCC2=CC=C(Cl)C=C2)C=CS1)N[C@H](C3=CC=CC=C3)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (134.45 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6890 mL 13.4452 mL 26.8904 mL
5 mM 0.5378 mL 2.6890 mL 5.3781 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.90%

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6890 mL 13.4452 mL 26.8904 mL 67.2260 mL
5 mM 0.5378 mL 2.6890 mL 5.3781 mL 13.4452 mL
10 mM 0.2689 mL 1.3445 mL 2.6890 mL 6.7226 mL
15 mM 0.1793 mL 0.8963 mL 1.7927 mL 4.4817 mL
20 mM 0.1345 mL 0.6723 mL 1.3445 mL 3.3613 mL
25 mM 0.1076 mL 0.5378 mL 1.0756 mL 2.6890 mL
30 mM 0.0896 mL 0.4482 mL 0.8963 mL 2.2409 mL
40 mM 0.0672 mL 0.3361 mL 0.6723 mL 1.6806 mL
50 mM 0.0538 mL 0.2689 mL 0.5378 mL 1.3445 mL
60 mM 0.0448 mL 0.2241 mL 0.4482 mL 1.1204 mL
80 mM 0.0336 mL 0.1681 mL 0.3361 mL 0.8403 mL
100 mM 0.0269 mL 0.1345 mL 0.2689 mL 0.6723 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AS1949490
Cat. No.:
HY-18686
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