[CAS NO. 1809085-30-0] VU0650786
PRODUCTS SPECIFICATIONS [1809085-30-0]
DESCRIPTION [1809085-30-0]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 387.80 |
| Molecular Formula | C18H15ClFN5O2 |
| SMILES | ClC1=CN=C(OCC2=NN([C@H](C)CN(C3=C(F)N=CC=C3)C4=O)C4=C2)C=C1 |
Summary
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) , with an IC 50 of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents [1] .
IC50 & Target
|
mGluR3 392 nM (IC 50 ) |
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) |
| t 1/2 (min) | 42 |
| CL plasma (mL/min/kg) | 37 |
| V SS (L/kg) | 1.6 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 250 mg/mL ( 644.66 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.36 mM); Clear solution
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.
- [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.
