Art. -Nr.: HY-18686

AS1949490

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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.

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Reinheit: 99.69%
CAS. Nr.: 1203680-76-5
Formel: C₂₀H₁₈ClNO₂S
Molecular Weight:371.88

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

AS1949490 Chemical Structure

CAS. Nr.: 1203680-76-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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].

Alle Akt Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 1203680-76-5
Appearance Solid
Molecular Weight 371.88
Formel C₂₀H₁₈ClNO₂S
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Life Sci

Drugs targeting SHIP2 demonstrate potent antiproliferative effects irrespective of SHIP2 inhibition. [Abstract]

2024 Nov 15:357:123101. PMID: 39366554

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6890 mL

13.4452 mL

26.8904 mL

5 mM

0.5378 mL

2.6890 mL

5.3781 mL

10 mM

0.2689 mL

1.3445 mL

2.6890 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Suwa A, et, al. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. Br J Pharmacol. 2009 Oct;158(3):879-87. [Content Brief]

[2]. Suwa A, et, al. Glucose metabolism activation by SHIP2 inhibitors via up-regulation of GLUT1 gene in L6 myotubes. Eur J Pharmacol. 2010 Sep 10;642(1-3):177-82. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

AS1949490

1 Cited Publications

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Publications Citing Use of MedChemExpress (MCE) AS1949490

Alle Akt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AS1949490 Related Classifications

HY-18686 Related Classifications