| Size | Price | Stock | Qty |
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| 5mg |
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| Other Sizes |
| Targets |
TUG-1387 is a structural analog of the FFA4 (GPR120) antagonist AH-7614 but is specifically designed to lack activity at the FFA4 receptor. It serves as an inactive negative control compound for studies evaluating the function of FFA4. By using TUG-1387 as a comparator, researchers can distinguish the specific effects of FFA4 activation or blockade from non-specific or off-target effects of AH-7614. The compound does not bind to or activate FFA4 and is used as a control in FFA4 functional evaluations.
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| ln Vitro |
In vitro, TUG-1387 is an analog of both AH-7614 and TUG-1506 that has no activity at FFA4 (GPR120). In FFA4 functional assays (e.g., calcium mobilization assays using FFA4-expressing cells), treatment with TUG-1387 (up to 100 uM) does not induce receptor activation (no increase in intracellular calcium) and does not antagonize the effects of FFA4 agonists such as TUG-891 or AH-7614. It serves as a negative control in cell-based assays to confirm that the observed effects of AH-7614 are mediated through FFA4 and not due to non-specific or off-target interactions. TUG-1387 is inactive on FFA4 and can be used as a negative control (NC) for FFA4 functional evaluation.
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| ln Vivo |
TUG-1387 is not used as a therapeutic agent and does not have in vivo biological activity on its own. It is a negative control compound for research studies. In pharmacological experiments in animals, TUG-1387 may be administered as a control treatment to compare against the effects of the active FFA4 antagonist AH-7614. For example, if AH-7614 produces a certain effect (e.g., inhibition of insulin secretion, modulation of gut hormone release), TUG-1387 should not produce that effect, confirming that the effect is specifically mediated by FFA4 blockade. The compound is not intended for therapeutic use and is not a drug candidate.
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| Enzyme Assay |
For non-cell-based binding assays, a standard protocol for measuring FFA4 binding uses a radioligand binding assay or a GTPgammaS binding assay with membranes prepared from cells expressing FFA4/GPR120. Varying concentrations of TUG-1387 (0.01-10,000 nM) are incubated with the membranes and a fixed concentration of a radiolabeled FFA4 ligand (e.g., [3H]TUG-891). After incubation, bound radioactivity is separated by filtration, and non-specific binding is determined. A competitive binding curve is generated; for an inactive negative control such as TUG-1387, no displacement of the radiolabeled ligand above background should be observed (IC50 >10 uM or no inhibition). For GTPgammaS assays, membranes are incubated with varying concentrations of TUG-1387 (0.1-10,000 nM) and [35S]GTPgammaS in assay buffer. The EC50 for receptor activation is calculated; for an inactive compound, no increase in bound radioactivity should be observed.
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| Cell Assay |
For in vitro cell-based assays, FFA4-expressing HEK293 cells (or another cell line stably expressing human FFA4/GPR120) are seeded in 96-well plates at 4 × 10^4 cells/well. Cells are loaded with the calcium-sensitive dye Fluo-4 AM (2-5 uM) in HBSS with 20 mM HEPES, 0.1% BSA, and 2.5 mM probenecid for 60 min at 37degC. After washing, cells are treated with varying concentrations of TUG-1387 (0.1-100 uM) and fluorescence (Ex 485 nm, Em 525 nm) is measured immediately. For inactive control experiments, no increase in intracellular calcium is observed. For antagonist assays, cells are pre-incubated with TUG-1387 (0.1-100 uM) for 15 min, followed by stimulation with an FFA4 agonist (e.g., TUG-891, 1 uM), and the inhibition of the agonist-induced calcium signal is measured. For an inactive control, TUG-1387 should not inhibit the agonist-induced calcium signal. The data demonstrate that TUG-1387 can serve as a negative control for studies assessing FFA4 function.
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| Animal Protocol |
TUG-1387 is not used directly in animal studies for therapeutic applications. It can be used as a negative control in pharmacokinetic/pharmacodynamic (PK/PD) studies or efficacy studies of FFA4 modulators. For example, in a mouse study evaluating the effects of the FFA4 antagonist AH-7614 on glucose tolerance, a separate group of mice would be treated with TUG-1387 (the inactive analog) at the same dose (e.g., 30 mg/kg, oral or intraperitoneal) as a control. TUG-1387 should not affect glucose tolerance or insulin secretion, confirming that any effect observed with AH-7614 is specifically mediated by FFA4. The protocol for such studies would mirror that of the active comparator, with the key difference being the use of the inactive negative control.
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| ADME/Pharmacokinetics |
TUG-1387 has a molecular weight of 315.37 g/mol and a molecular formula of C21H17NO2. The compound has moderate lipophilicity (cLogP ~5.0) and is soluble in DMSO (2 mg/mL, 6.34 mM). Pharmacokinetic data is not available, as the compound is not intended for therapeutic development and is used as a negative control. As a negative control, it is administered at the same dose and route as the active comparator (e.g., AH-7614) in control experiments, but no biological activity is expected. The half-life and clearance are likely similar to those of the active analog due to structural similarity.
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| Toxicity/Toxicokinetics |
TUG-1387 is an inactive negative control compound and is not intended for human use. Specific toxicity data for this compound is not publicly available, as it is not being developed for therapeutic applications. In cell viability assays, TUG-1387 is expected to have low toxicity at concentrations up to 100 uM, consistent with its lack of activity at FFA4 and expected low off-target reactivity. In animal studies, the compound is likely well tolerated at typical control doses (e.g., 10-50 mg/kg) when used as a negative control, but no formal toxicology studies have been conducted. Standard chemical safety precautions (gloves, lab coat, eye protection) should be followed.
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| References | |
| Additional Infomation |
TUG-1387 is a research compound and is not approved for clinical use. FFA4 (GPR120) is a receptor for long-chain fatty acids that has emerged as a therapeutic target for the treatment of metabolic diseases, including type 2 diabetes and obesity. FFA4 activation promotes GLP-1 secretion, improves insulin sensitivity, and reduces inflammation, making FFA4 agonists potential candidates for drug development. TUG-1387 was reported in the literature as a probe-dependent negative allosteric modulator of FFA4 (Watterson KR et al., Mol Pharmacol. 2017 Jun;91(6):630-641; Milligan G et al., Trends Pharmacol Sci. 2017 Sep;38(9):809-821). However, its primary use is as a negative control. This compound is an essential tool for validating FFA4 pharmacology and for distinguishing specific receptor-mediated effects from non-specific effects in cell-based and animal studies. This product is for research use only.
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| Molecular Formula |
C21H17NO2
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| Molecular Weight |
315.36518
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| Exact Mass |
315.126
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| CAS # |
6319-64-8
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| PubChem CID |
233017
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| Appearance |
White to off-white powder
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| Density |
1.25g/cm3
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| Boiling Point |
503.9ºC at 760 mmHg
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| Flash Point |
258.6ºC
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| Index of Refraction |
1.669
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| LogP |
5.011
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
421
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)C(=O)NC2C3=CC=CC=C3OC4=CC=CC=C24
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| InChi Key |
RWLHMQMVSKQATK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H17NO2/c1-14-10-12-15(13-11-14)21(23)22-20-16-6-2-4-8-18(16)24-19-9-5-3-7-17(19)20/h2-13,20H,1H3,(H,22,23)
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| Chemical Name |
4-methyl-N-(9H-xanthen-9-yl)benzamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1709 mL | 15.8544 mL | 31.7088 mL | |
| 5 mM | 0.6342 mL | 3.1709 mL | 6.3418 mL | |
| 10 mM | 0.3171 mL | 1.5854 mL | 3.1709 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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