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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C20H17FN4O2
- 分子量:364.37
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
hmGluR3 36 nM (EC50) |
体外実験
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.
Parmacokinetics
| 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 |
体内実験
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.
化学情報
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分子量 364.37
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分子式 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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別名
BI’7927
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
VU6052959 関連分類
HY-187356 関連分類
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