APD668 (Synonyms: JNJ-28630368) |
カタログ番号GC12738
One-Click Copy Product Info
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APD668 は、G タンパク質共役受容体 GPR119 の強力で選択的な経口活性アゴニストであり、hGPR119 と rGPR119 の EC50 はそれぞれ 2.7 nM と 33 nM です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 832714-46-2
Sample solution is provided at 25 µL, 10mM.
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APD688 is a selective and potent G protein-coupled receptor 119 (GPR119) agonist with an EC50 value of 2.7 nM for hGPR119 and 33 nM for rGPR119, and showed a moderate inhibition of the hERG channel (IC50 = 3 ?M), exhibiting an in vivo activity of glucose regulation in rodent models [1].
GPR199, which is predominantly expressed in human and rodent pancreas, is a membrane receptor that plays a role in the production of insulin as a response to high glucose concentration in male Wistar rats, and is a probable target for the treatment of diabetes [2]. GPR199 is also localized in the gastrointestinal track, providing a potential target for obesity therapy and other related metabolic disorders through reduced food intake [3].
In HEK293 cells transfected with human GPR119, application of APD688 displayed an increase in adenylatecyclase activation subsequently leading to enhanced release of insulin in a glucose-dependent manner [1].
Oral administration of APD688 in Zucker Diabetic Fatty (ZDF) rats for over 8 weeks resulted in the significant decrease in blood glucose and glycated hemoglobin (HbA1c) levels. In addition, the compound is mostly non-genotoxic, and shows no significant inhibition of CYP isoforms except for CYP2C9 (Ki = 0.1 ?M) in human hepatic microsomes [1].
References:
[1]. Semple G, Ren A, Fioravanti B, et al. Discovery of fused bicyclic agonists of the orphan G-protein coupled receptor GPR119 with in vivo activity in rodent models of glucose control. Bioorg Med Chem Lett, 2011, 21(10):3134-41.
[2]. Soga T, Ohishi T, Matsui T, et al. Lysophosphatidylcholine enhances glucose-dependent insulin secretion via an orphan G-protein-coupled receptor. Biochem Biophys Res Commun, 2005, 326(4):744-51.
[3]. Overton HA, Babbs AJ, Doel SM, et al. Deorphanization of a G protein coupled receptor for oleoylethanolamide and its use in the discovery of small molecule hypophagic agents. Cell Metab, 2006, 3(3):167-75.
| Cas No. | 832714-46-2 | SDF | |
| 同義語 | JNJ-28630368 | ||
| Formula | C21H24FN5O5S | M.Wt | 477.51 |
| 溶解度 | ≥ 17.4mg/mL in DMSO | Storage | Store at -20°C |
| 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. |
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| 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 | 2.0942 mL | 10.471 mL | 20.942 mL |
| 5 mM | 418.8 μL | 2.0942 mL | 4.1884 mL |
| 10 mM | 209.4 μL | 1.0471 mL | 2.0942 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)