VU6052959
VU6052959 (BI’7927) is an orally active, blood-brain barrier-penetrant mGlu3 modulator with an EC50 of 36 nM in humans and 16 nM in rats. VU6052959 enhances recognition memory and reverses cognitive impairment in male rats. VU6052959 can be used in the research of schizophrenia.
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- Fòrmula: C20H17FN4O2
- Peso molecular:364.37
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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hmGluR3 36 nM (EC50) |
VU6052959 is a potent positive allosteric modulator of human mGlu3 in GIRK cell-based assays, with an EC50 of 36 nM and a Glumax of up to 79%[1].
VU6052959 is a potent positive allosteric modulator of rat mGlu3, with an EC50 of 16 nM and a Glumax of 65% in cell-based assays[1].
VU6052959 (0-30 μM) exhibits extremely weak inhibitory effects on human CYP450 enzymes, with IC50 values >30 μM for CYP1A2, CYP2D6 and CYP3A4, and an IC50 value of 16 μM for CYP2C9[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CLplasma | T1/2 | MRT | Vss |
|---|---|---|---|---|---|---|
| Rat[1] | 0.2 mg/kg | i.v. | 19.8 mL/min/kg | 0.8 | 0.9 | 1.1 L/kg |
VU6052959 (3-30 mg/kg; p.o.; single administration) dose-dependently reverses cognitive impairment induced by MK-801 (HY-15084B) and Scopolamine (HY-N0296) in male Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose; 30 minutes prior to object exposure
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Result:Significantly enhanced recognition index compared to vehicle control at 10 mg/kg.
Produced a larger, highly significant enhancement in recognition index compared to vehicle control at 30 mg/kg.
Reached unbound brain levels of 50.1 nM (≈3.1-fold the rat mGlu3 PAM EC50) at 10 mg/kg.
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Animal Model:Sprague-Dawley (male; MK-801-induced cognitive impairment)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently reversed MK-801-induced deficits in recognition memory.
Produced significant enhancements compared to vehicle + MK-801 control at 3 mg/kg and 10 mg/kg.
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Animal Model:Sprague-Dawley (male; Scopolamine-induced cognitive impairment)[1]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose
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Result:Significantly reversed scopolamine-induced deficits in recognition memory compared to vehicle + scopolamine control at 10 mg/kg.
Produced a larger, highly significant reversal compared to vehicle + scopolamine control at 30 mg/kg.
Chemical Information
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Peso molecular 364.37
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Fòrmula C20H17FN4O2
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SMILES
FC1=CC=CC([C@H]2COC(C=C(NC(C3=NC=CC=N3)=O)C=C4)=C4N2C)=C1
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Synonyms
BI’7927
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
VU6052959 Related Classifications
HY-187356 Related Classifications
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