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FPTQ is novel and potent antagonist of mGluR1 (metabotropic glutamate receptor subtype 1) with IC50 of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. It may be applied as a ligand for positron emission tomography to visualize the rat brain's metabotropic glutamate receptor type 1 (mGluR1). FPTQ exhibited high specific binding with mGluR1 in the rat brain, according to in vitro autoradiography. FPTQ had a high uptake in the rat brain, according to a biodistribution study that used small-animal PET and the dissection method. Unlabeled FPTQ and mGluR1-selective ligand JNJ-16259685 decreased the uptake of radioactivity in the cerebellum, suggesting that FPTQ had mGluR1-specific binding in vivo. Due to the brain's low concentration of radiolabeled metabolites, FPTQ may have limited use in mGluR1 in vivo PET imaging.
| Targets |
Human mGluR1 ( IC50 = 6 nM ); Mouse mGluR1 ( IC50 = 1.4 nM )
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| ln Vitro |
FPTQ (0.5–10 μM) did not exhibit any cytotoxicity at 0.5, 1, 5, or 10 μM in RAW264.7 macrophage cells[2].
FPTQ (1–20 μM; 24 hours) decreases LPS-induced NO production at > 1 μM, and at 10 μM, FPTQ treatment has a 31% anti-oxidant effect in RAW264.7 macrophage cells[2]. FPTQ (1–20 μM; 24 hours) significantly reduces the levels of IL-1β and IL-6 expression induced by LPS. When FPTQ is added to RAW264.7 macrophage cells at a concentration of 10 μM, the mRNA expression of IL-1β and Il-6 is reduced by 27% and 44%, respectively[2]. |
| ln Vivo |
FPTQ (5-20 μM) reduces the quantity of neutrophils that migrate to the site of amputation in zebrafish larvae by tail amputation. The quantity of neutrophils aggregating at the wound site in zebrafish using the tailfin wound method likewise declines in a dose-dependent manner[2]. The Tg(mpx:EGFP)i114 zebrafish larvae are used in an LPS-induced inflammation zebrafish model. The larvae are introduced to FPTQ treatment right away after an injection of LPS solution into their yolks.
FPTQ (20 μM; 4 hours) has an anti-inflammatory effect in the early stages of inflammation and dramatically reduces fluorescent neutrophils following yolk injection[2].
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| Cell Assay |
Cell Line: RAW264.7 macrophage cells
Concentration: 1, 10, or 20 μM Incubation Time: 24 hours Result: Decreased IL-1β and IL-6 mRNA expression |
| References |
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| Molecular Formula |
C17H12FN5
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|---|---|
| Molecular Weight |
305.309085845947
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| Exact Mass |
305.11
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| CAS # |
864863-72-9
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| Related CAS # |
1025802-62-3; or 864863-72-9
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| Appearance |
Light yellow to yellow solid powder
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| SMILES |
CC1=C(N=NN1C2=C(N=CC=C2)F)C3=CC4=C(C=C3)N=CC=C4
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| InChi Key |
RTUBNVSZHGWRCV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H12FN5/c1-11-16(13-6-7-14-12(10-13)4-2-8-19-14)21-22-23(11)15-5-3-9-20-17(15)18/h2-10H,1H3
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| Chemical Name |
6-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]quinoline
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| Synonyms |
FPTQ
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2754 mL | 16.3768 mL | 32.7536 mL | |
| 5 mM | 0.6551 mL | 3.2754 mL | 6.5507 mL | |
| 10 mM | 0.3275 mL | 1.6377 mL | 3.2754 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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