(S)-Verapamil
Based on 1 Customer Validation
(S)-Verapamil ((S)-(-)-Verapamil) is an orally active MRP1 (ABCC1) modulator with a Kd value of 113 nM for hamster MRP1. (S)-Verapamil regulates MRP1, promotes MRP1-mediated glutathione efflux and the transport of calcein and leukotriene C4, reverses glutathione-activated MRP1 ATPase activity, and ultimately depletes intracellular glutathione and induces cell death. (S)-Verapamil specifically induces apoptosis in MRP1-overexpressing tumor cells. (S)-Verapamil can be used in research related to cancer, cardiac diseases such as supraventricular arrhythmia, and hypertension.
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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: 36622-29-4
- 分子式: C27H38N2O4
- 分子量:454.61
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Anti-Cardiovascular Disease Compound Library
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Orally Active Compound Library
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Apoptosis Compound Library
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Membrane Transporter/Ion Channel Compound Library
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Anti-Cancer Compound Library
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MES-SA/Dx5 | IC50 |
5.33 μM
Compound: Verapamil (S)
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TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
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[PMID: 12569305] |
(S)-Verapamil (72 h) potently induces cell death in MRP1-transfected BHK-21 cells[1].
(S)-Verapamil causes strong and rapid depletion of glutathione inside MRP1-transfected BHK-21 cells[1].
(S)-Verapamil (30 μM; 10 min) effectively inhibits MRP1-mediated calcein transport in MRP1-transfected BHK-21 cells[1].
(S)-Verapamil (1-256 μM; in the presence of 3 mM GSH), when combined with 3 mM GSH, potently inhibits ATP-dependent LTC4 transport in MRP1-transfected BHK-21 membrane vesicles[1].
(S)-Verapamil binds tightly to purified MRP1 with a Kd value of 113 nM, and induces significant conformational changes in purified MRP1[1].
(S)-Verapamil (4 h) slightly stimulates the basal ATPase activity of purified MRP1, and completely reverses the activation of ATPase activity induced by 5 mM GSH[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 36622-29-4
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性状 Oil
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分子量 454.61
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分子式 C27H38N2O4
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SMILES
[C@@](CCCN(CCC1=CC(OC)=C(OC)C=C1)C)(C(C)C)(C#N)C2=CC(OC)=C(OC)C=C2
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別名
(S)-(-)-Verapamil
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (219.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (protect from light). 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 (protect from light). 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
参考文献
[1]. Perrotton T, et al. (R)- and (S)-verapamil differentially modulate the multidrug-resistant protein MRP1. J Biol Chem. 2007;282(43):31542-31548. [Content Brief]
[2]. Busse D, et al. Cardiovascular effects of (R)- and (S)-verapamil and racemic verapamil in humans: a placebo-controlled study. Eur J Clin Pharmacol. 2006;62(8):613-619. [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 (protect from light). 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 | 2.1997 mL | 10.9984 mL | 21.9969 mL | 54.9922 mL |
| 5 mM | 0.4399 mL | 2.1997 mL | 4.3994 mL | 10.9984 mL | |
| 10 mM | 0.2200 mL | 1.0998 mL | 2.1997 mL | 5.4992 mL | |
| 15 mM | 0.1466 mL | 0.7332 mL | 1.4665 mL | 3.6661 mL | |
| 20 mM | 0.1100 mL | 0.5499 mL | 1.0998 mL | 2.7496 mL | |
| 25 mM | 0.0880 mL | 0.4399 mL | 0.8799 mL | 2.1997 mL | |
| 30 mM | 0.0733 mL | 0.3666 mL | 0.7332 mL | 1.8331 mL | |
| 40 mM | 0.0550 mL | 0.2750 mL | 0.5499 mL | 1.3748 mL | |
| 50 mM | 0.0440 mL | 0.2200 mL | 0.4399 mL | 1.0998 mL | |
| 60 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL | 0.9165 mL | |
| 80 mM | 0.0275 mL | 0.1375 mL | 0.2750 mL | 0.6874 mL | |
| 100 mM | 0.0220 mL | 0.1100 mL | 0.2200 mL | 0.5499 mL |
(S)-Verapamil 関連分類
HY-136907 関連分類
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