(R)-Verapamil
Based on 1 Customer Validation
(R)-Verapamil (Dexverapamil) is an optically enantiomer of the oral-active Verapamil (HY-14275). (R)-Verapamil has a relatively low affinity for L-type calcium channels (Cav1.2) (IC50 > 300 μM), and its IC50 for sodium channels (sodium channel) is 3.19 μM. (R)-Verapamil exhibits SSTR2 agonistic activity, with an EC50 of 1.3 μM. (R)-Verapamil significantly downregulates the expression of TXNIP protein in diabetic mouse models and significantly inhibits β-cell apoptosis (apoptosis), effectively controlling blood sugar. (R)-Verapamil can be used as a PET tracer for the function of P-glycoprotein (P-gp).
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。
- 純度: 98.97%
- CAS 番号: 38321-02-7
- 分子式: C27H38N2O4
- 分子量:454.60
-
保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
生物活性
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MES-SA/Dx5 | IC50 |
5.52 μM
Compound: Verapamil (R)
|
TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
TP_TRANSPORTER: drug resistance (paclitaxel) in MES-SA/DX5 cells
|
[PMID: 12569305] |
化学情報
-
CAS 番号 38321-02-7
-
性状 Oil
-
分子量 454.60
-
分子式 C27H38N2O4
-
Color Colorless to light yellow
-
SMILES
COC(C=C1CCN(C)CCC[C@](C#N)(C2=CC(OC)=C(C=C2)OC)C(C)C)=C(C=C1)OC
-
別名
Dexverapamil
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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 : 12.5 mg/mL (27.50 mM; ultrasonic and warming and heat to 60°C; 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 (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
-
データシート (272 KB)
-
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Chen YS, et al. Evaluating the antidiabetic effects of R-verapamil in type 1 and type 2 diabetes mellitus mouse models. PLoS One. 2021 Aug 6;16(8):e0255405. [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 Aug;62(8):613-9. [Content Brief]
[3]. Luurtsema G, et al. (R)- and (S)-[11C]verapamil as PET-tracers for measuring P-glycoprotein function: in vitro and in vivo evaluation. Nucl Med Biol. 2003 Oct;30(7):747-51. [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 | 10.9987 mL | 21.9974 mL | 54.9934 mL |
| 5 mM | 0.4399 mL | 2.1997 mL | 4.3995 mL | 10.9987 mL | |
| 10 mM | 0.2200 mL | 1.0999 mL | 2.1997 mL | 5.4993 mL | |
| 15 mM | 0.1466 mL | 0.7332 mL | 1.4665 mL | 3.6662 mL | |
| 20 mM | 0.1100 mL | 0.5499 mL | 1.0999 mL | 2.7497 mL | |
| 25 mM | 0.0880 mL | 0.4399 mL | 0.8799 mL | 2.1997 mL |