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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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VU6012962 is a novel, potent, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu7) negative allosteric modulator (NAM) with an IC50 of 347 nM. It reaches exposure in cerebral spinal fluid (CSF) 2.5 times higher than the in vitro IC50 at minimum effective doses (MEDs) of 3 mg/kg in preclinical anxiety models. It is suitable for use as an in vivo tool compound.
| Targets |
mGlu7 ( IC50 = 347 nM )
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|---|---|
| ln Vitro |
VU6012962 is highly mGlu7-specific in contrast to the other seven mGlu receptor subtypes[1].
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| ln Vivo |
VU6012962 (1–10 mg/kg; intraperitoneal injection; given 60 minutes before testing) reduces mice's anxiety in the elevated zero maze (EZM) test[1].
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| Animal Protocol |
C57Bl/6J male mice (8 weeks old)
1, 3, and 10 mg/kg I.p. injections; 60 minutes prior to testing |
| References |
| Molecular Formula |
C21H19F3N4O4
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|---|---|---|
| Molecular Weight |
448040
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| Exact Mass |
448.14
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| Elemental Analysis |
C, 56.25; H, 4.27; F, 12.71; N, 12.50; O, 14.27
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| CAS # |
2313526-86-0
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
COC1=C(C=CC(=C1)C(=O)NC2=C(C=CC(=C2)OC(F)(F)F)N3C=NC=N3)OCC4CC4
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| InChi Key |
IQNLJJLZIVCGFI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H19F3N4O4/c1-30-19-8-14(4-7-18(19)31-10-13-2-3-13)20(29)27-16-9-15(32-21(22,23)24)5-6-17(16)28-12-25-11-26-28/h4-9,11-13H,2-3,10H2,1H3,(H,27,29)
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| Chemical Name |
4-(cyclopropylmethoxy)-3-methoxy-N-[2-(1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl]benzamide
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| Synonyms |
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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 |
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| 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: ≥ 2.08 mg/mL (4.64 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 | 0.0022 mL | 0.0112 mL | 0.0223 mL | |
| 5 mM | 446.3887 nL | 0.0022 mL | 0.0045 mL | |
| 10 mM | 223.1944 nL | 0.0011 mL | 0.0022 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.
J Med Chem.2019 Jan 4. doi: 10.1021/acs.jmedchem.8b01810. |
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