Milameline
Milameline (CI-979; RU35926) is a nonselective, partical and orally active muscarinic receptor agonist that improves cognition. Milameline has equal affinity for different subtypes of human muscarinic receptors with IC50 of 1.3 µM for M1-, 1.1 µM for M2-, 1.5 µM for M3-, and 1.9 µM for M4-muscarinic receptors. Milameline has a higher affinity for sites [3H]CMD (IC50 = 20 nM), than [3H]QNB, (IC50 = 3059 nM). Milameline produces both central and peripheral cholinergic effects and reverses the cognitive deficits induced by Scopolamine (HY-N0296). Milameline can be used for the study of Alzheimer’s Disease.
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。
- CAS 番号: 139886-32-1
- 分子式: C8H14N2O
- 分子量:154.21
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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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mAChR1 1.3 μM (IC50) |
mAChR2 1.1 μM (IC50) |
mAChR3 1.5 μM (IC50) |
mAChR4 1.9 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.021 μM
Compound: Milameline
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Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
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[PMID: 25765911] |
Milameline increases soluble APP (sAPP) secretion in CHO cells transfected with human M1 or M3 receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Milameline (0.02- > 0.1 mg/kg, p.o.) effectively reverses Scopolamine (HY-N0296)-induced working memory impairment in rats at low doses (0.02-0.1 mg/kg), but the effect is reduced at high doses (> 0.1 mg/kg)[1].
Milameline increases cerebral blood flow in rats, and its distribution in the brain is consistent with the areas where the cholinergic system is enriched[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 139886-32-1
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分子量 154.21
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分子式 C8H14N2O
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SMILES
CO/N=C/C1=CCCN(C)C1
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別名
CI-979; RU35926
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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)