Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
FTIDC is a novel, orally bioactive, highly potent and selective negative allosteric modulator/antagonist of metabotropic glutamate receptor (mGluR) 1 with anxiolytic and antipsychotic effects. It blocks mGlu1 and mGlu5 with IC50 of 5.8 and 6200 nM, respectively. It may have therapeutic value for both humans and animal models. In the absence of ligand, it also functions as an inverse agonist of the mGlu1 receptor (IC50 = 7 nM). FTIDC inhibits L-glutamate-induced increases in intracellular calcium in mGlu1-expressing CHO cells and shows no effect at group II/III mGlu receptors. In vivo, it shows anxiolytic and antipsychotic effects in addition to inhibiting nociceptive behavior.
Targets |
mGluR1a ( IC50 = 5.8 nM ); mGlu5 ( IC50 = 6200 nM )
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ln Vitro |
FTIDC has IC50 values of 5.8 nM, 5.8 nM, 3.1 nM, and 7.7 nM for human mGluR1a, rat mGluR1a, mouse mGluR1a, and human mGluR1b in CHO cells, respectively, indicating that it inhibits the increase in intracellular Ca2+ concentrations caused by L-glutamate[1].
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ln Vivo |
FTIDC (i.p. or p.o.; 1-30 mg/kg) exhibits a statistically significant inhibitory effect on the duration of face-washing behavior elicited in a dose-dependent manner at doses of 10 and 30 mg/kg with i.p. and 30 mg/kg with p.o.[1].
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Animal Protocol |
Male CD1 (ICR) mice of 6-weeks-old
1, 3, 10, and 30 mg/kg I.p. or p.o. |
References |
Molecular Formula |
C18H23FN6O
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Molecular Weight |
358.41322
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Exact Mass |
358.19
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Elemental Analysis |
C, 60.32; H, 6.47; F, 5.30; N, 23.45; O, 4.46
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CAS # |
873551-53-2
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Appearance |
Solid powder
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SMILES |
CC1=C(N=NN1C2=C(N=CC=C2)F)C3=CCN(CC3)C(=O)N(C)C(C)C
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InChi Key |
CJTLKLBSIFQKNT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H23FN6O/c1-12(2)23(4)18(26)24-10-7-14(8-11-24)16-13(3)25(22-21-16)15-6-5-9-20-17(15)19/h5-7,9,12H,8,10-11H2,1-4H3
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Chemical Name |
4-[1-(2-fluoropyridin-3-yl)-5-methyltriazol-4-yl]-N-methyl-N-propan-2-yl-3,6-dihydro-2H-pyridine-1-carboxamide
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Synonyms |
FTIDC
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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) |
DMSO: ≥ 100 mg/mL (~279.0 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.98 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline 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 | 2.7901 mL | 13.9505 mL | 27.9010 mL | |
5 mM | 0.5580 mL | 2.7901 mL | 5.5802 mL | |
10 mM | 0.2790 mL | 1.3951 mL | 2.7901 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.