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AP5

Catalog No.GC35364 Copy One-Click Copy Product Info

AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM).

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AP5 Chemical Structure

Cas No.: 1623194-37-5

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Sample solution is provided at 25 µL, 10mM.



Description of AP5

AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor[1]. EC50: 0.49±0.28 nM (GPR40 Receptor)[1]

AP5 is a potent and selective GPR40 AgoPAM that demonstrates excellent in vivo efficacy. In the GK rat oral glucose tolerance test (oGTT), oral administration of AP5 1 h before an oral dextrose challenge shows that AP5 significantly reduces blood glucose levels compared to the vehicle. AP5 is determined to be more efficacious in this model, demonstrating maximally efficacious glucose lowering at a plasma concentration of 4.9 μM at 10 mg/kg[1].

[1]. Chen HY, et al. Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS Med Chem Lett. 2018 Jun 14;9(7):685-690.

Chemical Properties of AP5

Cas No. 1623194-37-5 SDF
Canonical SMILES FC1=CC(C2=CC(OC)=NC=C2)=CC=C1[C@@H]3CCC(C=CC([C@H](C4CC4)[C@H](C)C(O)=O)=C5)=C5O3
Formula C28H28FNO4 M.Wt 461.52
Solubility Soluble 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of AP5

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1 mg 5 mg 10 mg
1 mM 2.1668 mL 10.8338 mL 21.6675 mL
5 mM 433.4 μL 2.1668 mL 4.3335 mL
10 mM 216.7 μL 1.0834 mL 2.1668 mL
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In vivo Formulation Calculator (Clear solution) of AP5

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

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Review for AP5

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

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