| Identification | Back Directory | [Name]
VU0650786 | [CAS]
1809085-30-0 | [Synonyms]
VU0650786
Pyrazolo[1,5-a]pyrazin-4(5H)-one, 2-[[(5-chloro-2-pyridinyl)oxy]methyl]-5-(2-fluoro-3-pyridinyl)-6,7-dihydro-7-methyl-, (7R)- | [Molecular Formula]
C18H15ClFN5O2 | [MOL File]
1809085-30-0.mol | [Molecular Weight]
387.8 |
| Chemical Properties | Back Directory | [Boiling point ]
587.4±50.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 250 mg/mL (644.66 mM);Water : < 0.1 mg/mL (insoluble) | [form ]
Solid | [pka]
0.99±0.22(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents[1]. | [in vivo]
VU0650786 (VU786) (i.p., 30 mg/kg) increases the proportion of c-Fos-positive cells by approximately 4-fold, enhances synaptic strength in cone cell subpopulations, weakens thalamocortical long-term depression (LTD), and reduces passive coping in acute models of antidepressant-like activity in inducible cFos-EGFP mice[2].
The pharmacokinetic parameters of VU0650786 (compound 106) in rats[1].
| Parameters | IV (0.2 mg/kg) | | t1/2 (min) | 42 | | CL plasma (mL/min/kg) | 37 | | VSS (L/kg) | 1.6 |
| [IC 50]
mGluR3: 392 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Engers JL, et al. Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents. J Med Chem. 2015 Sep 24;58(18):7485-500. DOI:10.1021/acs.jmedchem.5b01005
[2] Max E Joffe, et al. mGlu2 and mGlu3 Negative Allosteric Modulators Divergently Enhance Thalamocortical Transmission and Exert Rapid Antidepressant-like Effects. Neuron. 2020 Jan 8;105(1):46-59.e3. DOI:10.1016/j.neuron.2019.09.044 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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