ML252 hydrochloride
ML252 hydrochloride is a selective inhibitor of KCNQ2 (Kv7.2) channel with IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 hydrochloride also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 hydrochloride shows highly brain penetrant.
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- CAS 番号: 2309887-61-2
- 分子式: C20H25ClN2O
- 分子量:344.88
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
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KCNQ2 69 nM (IC50) |
KCNQ1 2.92 μM (IC50) |
KCNQ2/Q3 0.12 μM (IC50) |
KCNQ4 0.20 μM (IC50) |
CYP1A2 6.1 μM (IC50) |
CYP2C9 18.9 μM (IC50) |
CYP3A4 3.9 μM (IC50) |
CYP2D6 19.9 μM (IC50) |
ML252 (1 μM; 0-48 h) hydrochloride shows an intrinsic clearance and subsequent predicted hepativ clearance of 1720 mL/min/kd and 67.3 mL/min/kg, respectively, in rat hepatic microsomes[1].
ML252 (0.1-10 μM) hydrochloride inhibits the current of KCNQ2 at 0.3 μM, and completely inhibits the current at 1 μM in CHO-KCNQ2 cell line[1].
ML252 (30 μM; 48 h) hydrochloride has no acute toxicity to CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 2309887-61-2
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性状 Solid
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分子量 344.88
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分子式 C20H25ClN2O
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Color White to off-white
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SMILES
CC[C@@H](C1=CC=CC=C1)C(NC2=CC=CC=C2N3CCCC3)=O.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
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Yu H, et al. Identification of a novel, small molecule inhibitor of KCNQ2 channels. 2011 Oct 28 [updated 2013 Feb 25]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. [Content Brief]
[2]. Cheung YY, et al. Discovery of a series of 2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)acetamides as novel molecular switches that modulate modes of K(v)7.2 (KCNQ2) channel pharmacology: identification of (S)-2-phenyl-N-(2-(pyrrolidin-1-yl)phenyl)butanamide (ML252) as a potent, brain penetrant K(v)7.2 channel inhibitor. J Med Chem. 2012 Aug 9;55(15):6975-9. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ML252 hydrochloride 関連分類
HY-18063A 関連分類
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