A-935142
Based on 1 Customer Validation
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
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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。
- 純度: 98.77%
- CAS 番号: 1031335-85-9
- 分子式: C18H19F3N2O2
- 分子量:352.35
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
A-935142 shortens the action potential duration (APD90) in guinea pig atrial tissue and canine cardiac Purkinje fibers[1].
A-935142 shortens cardiac action potentials and enhances the amplitude of the hERG current in a concentration- and voltage-dependent manner. A-935142 (60μM) increases both outward and inward K(+) current as well as the slope conductance of the linear portion of the fully activated I-V relation. A-935142 significantly reduces the time constants τ of hERG channel activation at two example voltages (-10 mV: tau=100+/-17 ms vs. 164+/-24 ms, n=6, P<0.01; +30 mV: tau=16.7+/-1.8 ms vs. 18.9+/-1.8 ms, n=5, P<0.05) and shifts the voltage-dependence for hERG activation in the hyperpolarizing direction by 9 mV[2].
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 1031335-85-9
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性状 Solid
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分子量 352.35
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分子式 C18H19F3N2O2
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Color White to off-white
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SMILES
O=C(O)C[C@H]1CC[C@H](C2=CC=C(C3=NNC(C(F)(F)F)=C3)C=C2)CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 125 mg/mL (354.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ohno H, et al. Absorption, disposition, metabolism and excretion of [14C]mizagliflozin, a novel selective SGLT1 inhibitor, in rats. Xenobiotica. 2019 Apr;49(4):463-473. [Content Brief]
[2]. Liu X, et al.Characterization of A-935142, a hERG enhancer, in the presence and absence of standard hERG blockers. Life Sci. 2012 Apr 20;90(15-16):607-11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8381 mL | 14.1904 mL | 28.3809 mL | 70.9522 mL |
| 5 mM | 0.5676 mL | 2.8381 mL | 5.6762 mL | 14.1904 mL | |
| 10 mM | 0.2838 mL | 1.4190 mL | 2.8381 mL | 7.0952 mL | |
| 15 mM | 0.1892 mL | 0.9460 mL | 1.8921 mL | 4.7301 mL | |
| 20 mM | 0.1419 mL | 0.7095 mL | 1.4190 mL | 3.5476 mL | |
| 25 mM | 0.1135 mL | 0.5676 mL | 1.1352 mL | 2.8381 mL | |
| 30 mM | 0.0946 mL | 0.4730 mL | 0.9460 mL | 2.3651 mL | |
| 40 mM | 0.0710 mL | 0.3548 mL | 0.7095 mL | 1.7738 mL | |
| 50 mM | 0.0568 mL | 0.2838 mL | 0.5676 mL | 1.4190 mL | |
| 60 mM | 0.0473 mL | 0.2365 mL | 0.4730 mL | 1.1825 mL | |
| 80 mM | 0.0355 mL | 0.1774 mL | 0.3548 mL | 0.8869 mL | |
| 100 mM | 0.0284 mL | 0.1419 mL | 0.2838 mL | 0.7095 mL |