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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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VU0650786 is a novel, potent, selective and CNS permeable negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. In rodents, VU0650786 exhibits anxiolytic and antidepressant properties.
Targets |
mGluR3 ( IC50 = 392 nM )
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ln Vivo |
VU0650786 (VU786) (i.p., 30 mg/kg) diminishes thalamocortical long-term depression (LTD), decreases passive coping in acute models of antidepressant-like activity in inducible cFos-EGFP mice, and increases the proportion of c-Fos-positive cells by about 4-fold[2]. It also improves synaptic strength in cone cell subpopulations[2].
Viu0650786 (compound 106) in rats: pharmacokinetic characteristics[1]. |
References |
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Molecular Formula |
C₁₈H₁₅CLFN₅O₂
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Molecular Weight |
387.80
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Exact Mass |
387.09
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CAS # |
1809085-30-0
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Appearance |
White to off-white solid powder
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SMILES |
C[C@@H]1CN(C(=O)C2=CC(=NN12)COC3=NC=C(C=C3)Cl)C4=C(N=CC=C4)F
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InChi Key |
RXRVCJFGSOVYLG-LLVKDONJSA-N
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InChi Code |
InChI=1S/C18H15ClFN5O2/c1-11-9-24(14-3-2-6-21-17(14)20)18(26)15-7-13(23-25(11)15)10-27-16-5-4-12(19)8-22-16/h2-8,11H,9-10H2,1H3/t11-/m1/s1
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Chemical Name |
(7R)-2-[(5-chloropyridin-2-yl)oxymethyl]-5-(2-fluoropyridin-3-yl)-7-methyl-6,7-dihydropyrazolo[1,5-a]pyrazin-4-one
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Synonyms |
VU-0650786; VU 0650786; VU0650786
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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: ~250 mg/mL (~644.7 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.36 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 20.8 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: ≥ 2.08 mg/mL (5.36 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5786 mL | 12.8932 mL | 25.7865 mL | |
5 mM | 0.5157 mL | 2.5786 mL | 5.1573 mL | |
10 mM | 0.2579 mL | 1.2893 mL | 2.5786 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.
PFC slices were prepared and incubated with vehicle, VU6001966 (VU966; 3 μM), or VU0650786 (VU786; 10 μM) for 1-6 hours prior to whole-cell recordings. Neuron . 2020 Jan 8;105(1):46-59.e3. td> |
c-Fos-EGFP mice were administered vehicle, the mGlu2 NAM VU6001966 (VU966; 10 mg/kg), or the mGlu3 NAM VU0650786 (VU786; 30 mg/kg), 45 minutes prior to being sacrificed for slice electrophysiology. Neuron . 2020 Jan 8;105(1):46-59.e3. td> |