Basic information Safety Supplier Related

VU0650786

Basic information Safety Supplier Related

VU0650786 Basic information

Product Name:
VU0650786
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)-
  • inhibit,anxiolytic activity,antidepressant,Inhibitor,VU-0650786,mGlu3 NAM,VU0650786,mGluR,Metabotropic glutamate receptors,VU 0650786
  • (7R)-2-{[(5-chloropyridin-2-yl)oxy]methyl}-5-(2-fluoropyridin-3-yl)-7-methyl-4H,5H,6H,7H-pyrazolo[1,5-a]pyrazin-4-one
  • VU0650786, 10 mM in DMSO
CAS:
1809085-30-0
MF:
C18H15ClFN5O2
MW:
387.8
Mol File:
1809085-30-0.mol
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VU0650786 Chemical Properties

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
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VU0650786 Usage And Synthesis

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].

ParametersIV (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)

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

VU0650786Supplier

Shanghai Lollane Biological Technology Co.,Ltd.
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13816613772
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Shanghai EFE Biological Technology Co., Ltd.
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Shanghai Changyu Medical Technology Co. Ltd.
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+86-13301875428
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Fan De(Beijing) Biotechnology Co., Ltd.
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15911056312
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liming@bio-fount.com
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