规格 | 价格 | 库存 | 数量 |
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500mg |
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1g |
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5g |
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Other Sizes |
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靶点 |
Calcium channel
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体外研究 (In Vitro) |
TR-iBRB2 细胞对 EverFluor FL Verapamil (EFV) 的摄取被阳离子药物 Verapamil 以浓度依赖性方式阻断,IC50 为 98.0 μM [4]。
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体内研究 (In Vivo) |
除了控制房颤时的房室结反应外,口服维拉帕米还可用于预防房室折返性心动过速[2]。缺血前,将维拉帕米静脉注射至股静脉。冠状动脉闭合后 45 分钟内,维拉帕米(1 mg/kg)可显着降低室性心律失常的发生率,例如室性心动过速(VT)、心室颤动(VF)和室性早搏(PVC)。缺血性心脏导致心律失常总评分显着增加。维拉帕米 (1 mg/kg) 可显着抑制缺血引起的总心律失常评分增加 [5]。
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药代性质 (ADME/PK) |
Metabolism / Metabolites
Dexverapamil has known human metabolites that include 2-(3,4-dimethoxyphenyl)acetaldehyde, (R)-D-617, arverapamil, and (2R)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(4-hydroxy-3-methoxyphenyl)-2-(propan-2-yl)pentanenitrile. |
毒性/毒理 (Toxicokinetics/TK) |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Limited information indicates that maternal doses of verapamil up to 360 mg daily produce low levels in milk. Newborns may have detectable verapamil serum levels, but levels are low. Verapamil would not be expected to cause any adverse effects in breastfed infants, especially if the infant is older than 2 months. ◉ Effects in Breastfed Infants No adverse reactions have been reported among 3 infants aged 13 days, 8 weeks and 3 months who were exposed to verapamil in breastmilk. ◉ Effects on Lactation and Breastmilk Verapamil can cause hyperprolactinemia and galactorrhea. The clinical relevance of these findings in nursing mothers is not known. The maternal prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
参考文献 |
[1]. Gowarty JL, et al. Verapamil as a culprit of palbociclib toxicity. J Oncol Pharm Pract. 2019 Apr;25(3):743-746.
[2]. Krikler DM. Verapamil in arrhythmia. Br J Clin Pharmacol. 1986;21 Suppl 2:183S-189S. [3]. Zhou P, et al. Anti-arrhythmic effect of Verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013 Aug 12;8(8):e71567. [4]. Rehnqvist N,et al. Effects of metoprolol vs verapamil in patients with stable angina pectoris. The Angina Prognosis Study in Stockholm (APSIS). Eur Heart J. 1996 Jan;17(1):76-81. [5]. Kubo Y, et al. Blood-to-Retina Transport of Fluorescence-Labeled Verapamil at the Blood-Retinal Barrier. Pharm Res. 2018 Mar 12;35(5):93 |
其他信息 |
Dexverapamil is a 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile that has R configuration. It competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1, EC 3.6.3.44), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms. Dexverapamil exhibits lower calcium antagonistic activity and toxicity than racemic verapamil. It has a role as an EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor. It is a conjugate base of a dexverapamil(1+). It is an enantiomer of a (S)-verapamil.
Dexverapamil is the R-enantiomer of the calcium channel blocker verapamil. Dexverapamil competitively inhibits the multidrug resistance efflux pump P-glycoprotein (MDR-1), thereby potentially increasing the effectiveness of a wide range of antineoplastic drugs which are inactivated by MDR-1 mechanisms. This agent exhibits decreased calcium antagonistic activity and toxicity compared to racemic verapamil. (NCI04) A calcium channel blocker that is a class IV anti-arrhythmia agent. See also: Verapamil (annotation moved to). |
分子式 |
C26H36N2O4
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分子量 |
454.611g/mol
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精确质量 |
454.283
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元素分析 |
C, 70.88; H, 8.24; N, 6.36; O, 14.53
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CAS号 |
38321-02-7
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相关CAS号 |
Verapamil;52-53-9;Verapamil-d3 hydrochloride;Verapamil-d6 hydrochloride;1185032-80-7;Verapamil-d3-1 hydrochloride;2714485-49-9
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PubChem CID |
65808
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外观&性状 |
White to off-white solid powder
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熔点 |
129-131ºC
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折射率 |
1.529
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LogP |
5.093
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tPSA |
63.95
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氢键供体(HBD)数目 |
0
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氢键受体(HBA)数目 |
6
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可旋转键数目(RBC) |
13
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重原子数目 |
33
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分子复杂度/Complexity |
606
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定义原子立体中心数目 |
1
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SMILES |
CC(C)[C@@](CCCN(C)CCC1=CC(=C(C=C1)OC)OC)(C#N)C2=CC(=C(C=C2)OC)OC
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InChi Key |
FTZCBMKQDCJEKJ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H36N2O4/c1-7-26(19-27,21-12-13-22(29-3)24(18-21)31-5)15-9-16-28(2)17-14-20-10-8-11-23(30-4)25(20)32-6/h8,10-13,18H,7,9,14-17H2,1-6H3
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化学名 |
(+)-3-(3,4-Dimethoxyphenyl)-6-((5,6-dimethoxyphenethyl)methylamino)hexane-3-carbonitrile
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别名 |
Dexverapamil; Dexverapamilum; EINECS 253-878-4
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HS Tariff Code |
2934.99.9001
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month 注意: 请将本产品存放在密封且受保护的环境中(例如氮气保护),避免吸湿/受潮和光照。 |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外实验) |
DMSO : ≥ 10 mg/mL
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溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 5 mg/mL (10.18 mM) (饱和度未知) in 10% DMSO + 90% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
*生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.08 mg/mL (4.24 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 20.8 mg/mL澄清的DMSO储备液加入到400 μL PEG300中,混匀;再向上述溶液中加入50 μL Tween-80,混匀;然后加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.08 mg/mL (4.24 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 配方 4 中的溶解度: ≥ 2.08 mg/mL (4.24 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,您可以将 100 μL 20.8 mg/mL 澄清 DMSO 储备液添加到 900 μL 玉米油中并混合均匀。 配方 5 中的溶解度: 25 mg/mL (50.91 mM) in PBS (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液; 超声助溶. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。