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VU0422288

Catalog No. T29135   CAS 1630936-95-6
Synonyms: VU-0422288, ML-396, ML396, VU 0422288, ML 396

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).

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VU0422288 Chemical Structure
VU0422288, CAS 1630936-95-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 73.00
10 mg In stock $ 123.00
25 mg In stock $ 247.00
50 mg In stock $ 396.00
100 mg In stock $ 645.00
500 mg In stock $ 1,330.00
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Purity: 95.48%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 mGluR4:108 nM (EC50), mGluR7:146 nM (EC50), mGluR8:128 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].
Synonyms VU-0422288, ML-396, ML396, VU 0422288, ML 396
Molecular Weight 360.19
Formula C17H11Cl2N3O2
CAS No. 1630936-95-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/mL(55.53 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Gogliotti RG, et al. mGlu7 potentiation rescues cognitive, social, and respiratory phenotypes in a mouse model of Rett syndrome. Sci Transl Med. 2017 Aug 16;9(403):eaai7459. 2. Jalan-Sakrikar N, et al. Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor 7. ACS Chem Neurosci. 2014 Dec 17;5(12):1221-37.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library

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Keywords

VU0422288 1630936-95-6 Neuroscience GluR VU-0422288 ML-396 ML396 VU 0422288 ML 396 inhibitor inhibit

 

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