AS 1949490 |
| Catalog No.GC13516 |
Selective SHIP2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1203680-76-5
Sample solution is provided at 25 µL, 10mM.
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AS 1949490 is a selective inhibitor of Src homology 2 domain-containing inositol-5-phosphatase 2 (SHIP2), [1] with IC50 values of 0.34 µM and 0.62 µM to mouse and human SHIP2s, respectively [2].
SHIP2 is an intracellular phosphatase and appears to be important in insulin signaling as a negative regulator. SHIP2 has potential to act as a treatment for type 2 diabetes because of its inhibition [2].
Akt is a key enzyme to regulated insulin signaling. AS 1949490 treatment dose-dependently increased insulin-induced phosphorylation of Akt in L6 myotubes, but did not result in any associated changes in the overall level of Akt protein and the fetal bovine serum-induced phosphorylation of Akt. Treatments with AS 1949490 at several concentrations of and 1 nM insulin for 48 h, showed more consumption of glucose in the medium in a concentration-dependent manner [2].
In diabetic db/db mice, administered with AS 1949490 twice daily p.o. for 7 or 10 days significantly decreased plasma glucose (23% reduction, relative to vehicle), without affecting insulin levels, food intake or body weight. In the 10th day, treatment with AS 1949490 resulted in significant reduction in both the area under the blood glucose concentration time curve (AUC) and fasting blood glucose (37% reduction, compared with vehicle; time = -30 min) [2].
References:
[1]. Laura Beth J. McIntire, Kyu-In Lee, Belle Chang-IIeto, et al. Screening assay for small molecule inhibitors of synaptojanin 1, a synaptic phosphoinositide phosphatase. J Biomol Screen, 2014, 19(4):585-594.
[2]. A Suwa, T Yamamoto, A Sawada, et al. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. British Journal of Pharmacology, 2009, 158:879-887.
| Cas No. | 1203680-76-5 | SDF | |
| Chemical Name | (S)-3-((4-chlorobenzyl)oxy)-N-(1-phenylethyl)thiophene-2-carboxamide | ||
| Canonical SMILES | ClC1=CC=C(C=C1)COC2=C(C(N[C@@H](C)C3=CC=CC=C3)=O)SC=C2 | ||
| Formula | C20H18ClNO2S | M.Wt | 371.88 |
| Solubility | ≥ 11.6mg/mL in DMSO | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.689 mL | 13.4452 mL | 26.8904 mL |
| 5 mM | 0.5378 mL | 2.689 mL | 5.3781 mL |
| 10 mM | 0.2689 mL | 1.3445 mL | 2.689 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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