AH 7614 (Synonyms: NSC 31171，N-xanthen-9-yl-p-Toluenesulfonamide) |
| Katalog-Nr.GC17753 |
FFA4/GPR120 antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 6326-06-3
Sample solution is provided at 25 µL, 10mM.
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Target: FFA4/GPR120
IC50: N/A
AH7614 is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist with pIC50 values of 7.1, 8.1 and 8.1 at the human, mouse and rat receptor, respectively [1]. The free fatty acid receptor 4 (FFA4/GPR120), a member of the G protein-coupled receptor family, is a potential 7TM receptor involved in long-chain fatty acid-stimulated glucagon-like peptide-1 (GLP-1) secretion. FFA4 is highly expressed in the intestinal endocrine cell line STC-1 and the intestine. GLP-1 regulates multiple physiological functions including eating behavior [2].
In vitro: AH7614 (0.063, 0.25, and 1μM) blocked linoleic acid and GSK137647A-induced intracellular calcium increase in U2OS osteosarcoma cells expressing the FFA4 receptor [1]. In addition, the increase of glucose-stimulated insulin secretion by GSK137647A (50 μM) was abolished in the presence of the selective FFA4 antagonist AH7614 (100 μM) in the MIN6 mouse insulinoma cell line. Moreover, AH7614 (100 μM) blocked GSK137647A (100μM)-mediated a modest increase of GLP-1 secretion in the NCIH716 cells [1].
In vivo: N/A
References:
1. Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3.
2. Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res. 2012;53(11):2256-65.
| Cell experiment [1]: | |
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Cell lines |
Flp-In T-REx 293 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10-10 ~10-5 M for 15 minutes |
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Applications |
AH-7614 inhibited, in a potent and concentration-dependent manner, the ability of ω-3 fatty acid aLA to promote Ca2+ mobilization in Flp-In T-REx 293 cells induced to express hFFA4-eYFP. As an antagonist of FFA4, AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid |
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References: [1] Watterson KR, Hansen SVF, Hudson BD, et al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641. |
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| Cas No. | 6326-06-3 | SDF | |
| Überlieferungen | NSC 31171，N-xanthen-9-yl-p-Toluenesulfonamide | ||
| Chemical Name | 4-methyl-N-(9H-xanthen-9-yl)benzenesulfonamide | ||
| Canonical SMILES | O=S(NC1C2=C(C=CC=C2)OC3=CC=CC=C31)(C4=CC=C(C)C=C4)=O | ||
| Formula | C20H17NO3S | M.Wt | 351.42 |
| Löslichkeit | 30mg/mL in DMSO & DMF | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8456 mL | 14.228 mL | 28.456 mL |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 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 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 40 reference(s) in Google Scholar.)
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