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Catalog:
SLK-S2862
Brand:
Selleck
CAS:
61350-00-3
Overview
MDL
MFCD00548412
Molecular Weight
232.67
Molecular Formula
C12H9ClN2O
SMILES
O=C(C1=NC=CC=C1)NC2=CC=CC(Cl)=C2
For research use only.
Storage
3 years,-20°C,powder 1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
1 mg
5 mg
10 mg
1 mM
4.2979 mL
21.4897 mL
42.9793 mL
5 mM
0.8596 mL
4.2979 mL
8.5959 mL
10 mM
0.4298 mL
2.1490 mL
4.2979 mL
50 mM
0.0860 mL
0.4298 mL
0.8596 mL
Description
VU 0364770 is a positive allosteric modulator(PAM) of with of 1.1 μM, exhibits insignificant activity at 68 other receptors, including other mGlu subtypes.
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.
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.
