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VU0422288 (ML396) is a potent orthosteric modulator of type III mGlu receptors (mGlus).VU0422288 shows inhibition of mGluR4, mGluR7, and mGluR8 in a calcium mobilization assay.VU0422288 can be used to study Rett syndrome (RTT).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $73 | In Stock | |
10 mg | $123 | In Stock | |
25 mg | $247 | In Stock | |
50 mg | $396 | In Stock | |
100 mg | $645 | In Stock | |
500 mg | $1,330 | In Stock |
Description | VU0422288 (ML396) is a potent orthosteric modulator of type III mGlu receptors (mGlus).VU0422288 shows inhibition of mGluR4, mGluR7, and mGluR8 in a calcium mobilization assay.VU0422288 can be used to study Rett syndrome (RTT). |
Targets&IC50 | mGluR7:146 nM (EC50), mGluR8:128 nM (EC50), mGluR4:108 nM (EC50) |
In vitro | In coronal slices containing the hippocampus, VU0422288 (1 μM; 5 minutes) enhances the reduction in slope of the field excitatory postsynaptic potentials (fEPSPs) induced by 30 μM LSP4-2022[1].However, when administered alone for 10 minutes at a concentration of 1 μM, VU0422288 does not alter the slope of fEPSP, indicating that under stimulation conditions, mGlu7 does not possess reinforcing activity in Mecp2-/y slices[1]. |
In vivo | In Mecp2+/- mice, VU0422288 (30 mg/kg; intraperitoneal injection; once daily for 17 days) rescues synaptic plasticity deficits and learning-memory phenotypes, reduces the frequency of respiratory pause, while showing no effect in Mecp2+/+ animals[1]. A single dose of VU0422288 (10 mg/kg; intraperitoneal injection) in adult male Sprague-Dawley rats exhibits a plasma/brain partition coefficient of 1.67, predicting a free brain concentration of approximately 40 nM[1]. |
Alias | VU-0422288, VU 0422288, ML-396, ML396, ML 396 |
Molecular Weight | 360.19 |
Formula | C17H11Cl2N3O2 |
Cas No. | 1630936-95-6 |
Smiles | Clc1ccc(Oc2ccc(NC(=O)c3ccccn3)cc2Cl)nc1 |
Relative Density. | 1.445 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 3.6 mg/mL (10 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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