ML218 hydrochloride
Based on 2 publication(s) in Google Scholar
ML218 hydrochloride is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier.
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: 2319922-08-0
- 分子式: C19H27Cl3N2O
- 分子量:405.79
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
MedChemExpress（MCE）の使用を引用している文献 ML218 hydrochloride
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生物活性
製品説明
IC50 & Target
IC50: 310 nM (Cav3.2), 270 nM (Cav3.3), and 150 nM (Ca2+ flux)[1]
体外実験
In plasma protein binding studies (equilibrium dialysis), ML218 possesses good free fraction in both rat and human. Intrinsic clearance experiments in liver microsomes indicated that ML218 is highly cleared in rat (CLint = 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CLint = 12.7 mL/min/kg)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
Free brain and plasma concentrations of ML218 increases in a dose proportional manner across the dose range (3 mg/kg: [plasma] = 98 nM, [brain] = 1.66 μM; 10 mg/kg: [plasma] = 282 nM, [brain] = 5.03 μM; 30 mg/kg: 1.2 μM, [brain] = 17.7 μM)[1].
Noncompartmental pharmacokinetic analysis indicates ML218 (1 mg/kg, IV) has a mean residence time (MRT) of nearly 7 h, a value which is consistent with its terminal half-life (t1/2 = 7 h)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (275-299 g) induced by haloperidol[1]
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Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:Oral administration; once
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Result:Reversed cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol.
化学情報
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CAS 番号 2319922-08-0
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分子量 405.79
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分子式 C19H27Cl3N2O
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SMILES
O=C(NC[C@@H]1[C@@]2([H])CN(CCC(C)(C)C)C[C@@]12[H])C3=CC(Cl)=CC(Cl)=C3.[H]Cl
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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.
Publications (2)
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Journal Impact Factor
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Most Recent
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Biomaterials
Electroactive membranes enhance in-situ alveolar ridge preservation via spatiotemporal electrical modulation of cell motility. [Abstract]2025 Jun:317:123077. PMID: 39756273 -
Mol Genet Genomics
CACNA1H restrains chemotherapy resistance in ovarian clear cell carcinoma cells by repressing autophagy. [Abstract]2024 Aug 6;299(1):77. PMID: 39105964
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)
ML218 hydrochloride 関連分類
HY-103309A 関連分類
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