M4 mAChR Modulator-2
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC50 = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a Ki of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study 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。
- CAS 番号: 3062458-27-6
- 分子式: C26H24FN5O
- 分子量:441.50
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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]|
mAChR4 513 nM (EC50) |
mAChR4 377 nM (Ki) |
体外実験
M4 mAChR Modulator-2 (Compound A9) enhances acetylcholine-induced activation of M4 muscarinic acetylcholine receptors (M4 mAChR) (EC50 = 513 nM) in Cisbio IP-One Gq assay, showing potent M4 positive allosteric modulator (PAM) activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice[1]
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Dosage:10, 30, 60, 120 mg/kg
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Administration:p.o. administered 30 min before intraperitoneal injection of 0.3 mg/kg Dizocilpine (MK-801) (HY-15084B) for a single dose
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Result:Reversed MK-801-induced hyperlocomotion in male ICR mice with an ED₅₀ of 20.04 mg/kg (p.o.) when administered 30 min before intraperitoneal injection of 0.3 mg/kg MK-801, with locomotor activity recorded for 60 min.
Showed no adverse effects (including mortality, diarrhea, sedation, or gait abnormalities) in male ICR mice at the highest tested dose of 120 mg/kg.
化学情報
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CAS 番号 3062458-27-6
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分子量 441.50
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分子式 C26H24FN5O
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SMILES
CC1=C2C(CN(C(CC3CN(C4=CC(C5=CC=C(C#N)C(F)=C5)=NC=C4)C3)=O)C2)=NC(C)=C1
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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)
M4 mAChR Modulator-2 関連分類
HY-175532 関連分類
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