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VU6033685

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Catalog No. T205368

VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.

VU6033685

VU6033685

😃Good
Catalog No. T205368
VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.
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Bioactivity
Description
VU6033685 is an orally effective positive allosteric modulator (PAM) of mGlu1, capable of positively modulating human mGlu1 and mGlu5, with EC50 values of 39 nM and 3960 nM, respectively. Additionally, VU6033685 inhibits CYP1A2, CYP2C9, and CYP2D6 with IC50 values of 26, 22.3, and 23.8 μM. It reverses amphetamine-induced hyperactivity in rats and protects against MK-801-induced cognitive deficits. VU6033685 demonstrates favorable pharmacokinetic properties in rats, with an oral bioavailability of 42.8%.
Chemical Properties
Molecular Weight366.84
FormulaC20H19ClN4O
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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