BRD3290
BRD3290 is a GluA3-preferring AMPA receptor positive allosteric modulator with brain exposure in Mus musculus (mice) following peripheral administration. BRD3290 preferentially potentiates GluA3-containing AMPA receptors over GluA1/2-containing AMPA receptors. BRD3290 increases cerebellar cGMP levels in Mus musculus (mice). BRD3290 does not induce convulsions, alter motor function, or improve novel object recognition task performance in Mus musculus (mice) at tested doses. BRD3290 can be used for the research of schizophrenia.
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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: C20H27N3O3S
- 分子量:389.51
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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AMPA Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
3.7 μM
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Potentiation of GluA3i/2o AMPAR-mediated charge density in tetracycline-inducible HEK293T cells assessed by automated patch clamp electrophysiology assay with 48 h doxycycline induction, 3 min pre-incubation with BRD3290, and 500 ms glutamate puff at -80 mV voltage clamp.
Potentiation of GluA3i/2o AMPAR-mediated charge density in tetracycline-inducible HEK293T cells assessed by automated patch clamp electrophysiology assay with 48 h doxycycline induction, 3 min pre-incubation with BRD3290, and 500 ms glutamate puff at -80 mV voltage clamp.
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2026.07.26.740780 |
| HEK-293T | EC50 |
16.9 μM
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Potentiation of GluA1i/2o AMPAR-mediated charge density in tetracycline-inducible HEK293T cells assessed by automated patch clamp electrophysiology assay with 48 h doxycycline induction, 3 min pre-incubation with BRD3290, and 500 ms glutamate puff at -80 mV voltage clamp.
Potentiation of GluA1i/2o AMPAR-mediated charge density in tetracycline-inducible HEK293T cells assessed by automated patch clamp electrophysiology assay with 48 h doxycycline induction, 3 min pre-incubation with BRD3290, and 500 ms glutamate puff at -80 mV voltage clamp.
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2026.07.26.740780 |
In FLIPR calcium flux assays, BRD3290 (0.068 μM; induced by 48 h Doxycycline (HY-N0565)) exhibits 10-fold higher activity in HEK293T cells expressing GluA3i/2o than in those expressing GluA1i/2o[1].
BRD3290 (10 nM-100 µM; 48 h Doxycycline induction, 3 min pre-incubation) enhances GluA3i/2o AMPAR with an EC50 of 3.7 µM; in automated patch-clamp electrophysiology assays using HEK293T cells, its activity is 10.9-fold higher than that of GluA1i/2o AMPAR (EC50 = 16.9 µM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BRD3290 (10-100 mg/kg; i.p.; single administration) does not induce convulsions in healthy male C57BL/6J mice[1].
BRD3290 (3-56 mg/kg; i.p.; single administration) does not induce motor impairment in healthy wild-type mice as detected by the accelerated rotarod test[1].
BRD3290 (3-56 mg/kg; i.p.; two administrations with a 24 h interval) exerts no improving effect on the performance of healthy wild-type mice in the 24 h novel object recognition task[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (male, aged P80-P100, weighing 25-35g)[1]
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Dosage:56 mg/kg
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Administration:i.p.; single dose
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Result:Increased cerebellar cGMP levels relative to vehicle-treated mice.
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Animal Model:C57BL/6J (male, aged 3-5 months)[1]
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Dosage:10, 30, 56 mg/kg
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Administration:i.p.; single dose
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Result:Did not induce convulsions at any tested dose.
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Animal Model:Wild-type[1]
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Dosage:10, 30, 56 mg/kg
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Administration:i.p.; single dose
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Result:Did not significantly alter rotarod fall latency relative to vehicle-treated mice at any tested dose.
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Animal Model:Wild-type[1]
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Dosage:3, 10, 30, 56 mg/kg
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Administration:i.p.; two doses, 24 hours apart
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Result:Did not increase the time spent exploring the novel object relative to the familiar object at any tested dose.
化学情報
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分子量 389.51
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分子式 C20H27N3O3S
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SMILES
CC(C)S(N[C@H]1CNCC[C@@H]1C(C=C2)=CC=C2C3=CC=CC(O)=C3N)(=O)=O
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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)