Home Neuronal Signaling GluR agonist VU 0364770

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VU 0364770 GluR agonist

Cat.No.S2862

VU 0364770 is a positive allosteric modulator(PAM) of mGlu4 with EC50 of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
VU 0364770 GluR agonist Chemical Structure

Chemical Structure

Molecular Weight: 232.67

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Quality Control

Batch: S286201 DMSO]47 mg/mL]false]Ethanol]47 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Chemical Information, Storage & Stability

Molecular Weight 232.67 Formula

C12H9ClN2O

 Storage (From the date of receipt)
CAS No. 61350-00-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1=CC=NC(=C1)C(=O)NC2=CC(=CC=C2)Cl

Solubility

In vitro
Batch:

DMSO : 47 mg/mL (202.0 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 47 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
mGlu4 [1]
1.1 μM(EC50)
In vitro
VU0364770 is a potent and effective positive allosteric modulator of mGlu4. VU0346770 exhibits a potency of 1.1 ± 0.2 μM at human mGlu4 in the presence of an EC20 concentration of glutamate and shifts the glutamate concentration-response curve 31.4 ± 4.0-fold to the left. VU0364770 exhibits a potency of 290 ± 80 nM at rat mGlu4 and induces an 18.1 ± 1.7-fold left shift of the glutamate concentration-response curve. [1]
In vivo
VU0364770 shows efficacy alone or when administered in combination with l-DOPA or an adenosine 2A (A2A) receptor antagonist preladenant currently in clinical development. When administered alone, VU0364770 exhibits efficacy in reversing haloperidol-induced catalepsy, forelimb asymmetry-induced by unilateral 6-hydroxydopamine (6-OHDA) lesions of the median forebrain bundle, and attentional deficits induced by bilateral 6-OHDA nigrostriatal lesions in rats. In addition, VU0364770 enhances the efficacy of preladenant to reverse haloperidol-induced catalepsy when given in combination. The effects of VU0364770 to reverse forelimb asymmetry are also potentiated when the compound is coadministered with an inactive dose of l-DOPA, suggesting that mGlu4 positive allosteric modulator may provide l-DOPA-sparing activity. [1]
References

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