VU0650786 manufacturers
- VU0650786
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- $97.00 / 1mg
-
2024-11-19
- CAS:1809085-30-0
- Min. Order:
- Purity: 98.96%
- Supply Ability: 10g
- VU0650786
-
- $97.00 / 1mg
-
2024-11-19
- CAS:1809085-30-0
- Min. Order:
- Purity: 98.96%
- Supply Ability: 10g
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| | 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 | | EINECS: | | | Product Categories: | | | Mol File: | 1809085-30-0.mol |  |
| | 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 |
| | 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].
| 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) | | 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 |
| | VU0650786 Preparation Products And Raw materials |
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