Chemical Structure : VU6081679
CAS No.:
VU6081679
(VU 6081679)
Catalog No.: PC-27729Not For Human Use, Lab Use Only.
VU6081679 is a potent, CNS penetrant, orally bioavailable metabotropic glutamate receptor subtype 8 (mGlu8) positive allosteric modulator (PAM) with EC50 of 211/190/162 nM for rat/mouse/human Glu8 receptors respectively.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
VU6081679 is a potent, CNS penetrant, orally bioavailable metabotropic glutamate receptor subtype 8 (mGlu8) positive allosteric modulator (PAM) with EC50 of 211/190/162 nM for rat/mouse/human Glu8 receptors respectively.
VU6081679 is selective over CNS expressed Group III mGlus, mGlu4 and mGlu7, as well as the Group II mGlus, mGlu2 and mGlu3.
VU6081679 displays weak PAM activity at the two Group I mGlu receptors (mGlu1 EC50 = 295 nM (42% Glu Max); mGlu5 EC50 = 1290 nM (49% Glu Max)).
VU6081679 displays a good rodent PK profile, allowing for in vivo evaluation.
VU6081679 exhibits efficacy in an acute haloperidol-induced catalepsy model of Parkinson's disease in two rodent species.
Physicochemical Properties
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M.Wt
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421.43
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Formula
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C22H20FN5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6-(3,4-Dimethoxyphenyl)-2-((5-fluoro-6-(1-methyl-1H-pyrazol-4-yl)pyridin-3-yl)methyl)pyridazin-3(2H)-one
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References
1. Alexa E Richardson, et al. ACS Chem Neurosci. 2026 Aug 5;17(15):3023-3034.
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