VU6033685
VU6033685 is the orally active positive allosteric modulator (PAM) for mGlu1 that positively modulates human mGlu1 and human mGlu5 with EC50 of 39 nM and 3960 nM. VU6033685 also inhibits CYP1A2, CYP2C9 and CYP2D6 with IC50 of 26, 22.3 and 23.8 μM, respectively. VU6033685 reverses amphetamine-induced rats hyperlocomotion, protects rats from MK-801 (HY-15084B)-induced cognitive impairment. VU6033685 exhibits good pharmacokinetics characteristics in rats with an oral bioavailability of 42.8%.
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- 화학식: C20H19ClN4O
- 분자량:366.84
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
EC50: human mGlu5 (39 nM); human mGlu5 (3960 nM)
IC50: CYP1A2 (26 μM); CYP2C9 (22.3 μM); CYP2D6 (23.8 μM)
Chemical Information
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분자량 366.84
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화학식 C20H19ClN4O
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SMILES
CC1=NC(C2CC2)=CC=C1CNC(C3=CC(N4C=CC=N4)=CC=C3Cl)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)