Verapamil HCl | CP-16533-1 hydrochloride;Verapamil (hydrochloride);NSC 657799;NSC 272366;(±)-Verapamil;CP-16533-1;Verapamil HCl;(±)-Verapamil hydrochloride | Drug Standard | Other Compounds | Calcium Channel

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盐酸维拉帕米 /Verapamil HCl {[allProObj[0].p_purity_real_show]}

货号：A724474 同义名： CP-16533-1 hydrochloride;Verapamil (hydrochloride)

Verapamil HCl is a phenylalkylamine class L-type calcium channel blocker.

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Verapamil HCl 化学结构
CAS号：152-11-4

Verapamil HCl 3D分子结构
CAS号：152-11-4

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Verapamil HCl 纯度/质量文件产品仅供科研

货号：A724474 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 更多 >

Calcium Channel 亚型比较

产品名称	Ca2+ channel-like protein ↓ ↑	Calcium Channel ↓ ↑	Cav 2.2 ↓ ↑	其他靶点	纯度
CDC25B-IN-2	✔			Akt	99%+
Clevidipine		✔			97%
Verapamil HCl		✔			99%
Amlodipine		✔			99%
Amlodipine maleate		✔			98%
(+)-cis-Diltiazem HCl		✔			95%
Zegocractin		++ Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM			99%+
Tanshinone IIA sulfonate sodium		✔			98%
Ulixacaltamide		++ hCaV3.1, IC50: 50 nM hCaV3.2, IC50: 110 nM			99%+
Dronedarone Hydrochloride		✔			95%
Nitrendipine		+ Calcium channel, IC50: 95 nM			98%
Efonidipine HCl monoethanolate		✔			98%
Cinnarizine		✔			98%
SEA0400		++ NCX, IC50: 33 nM		ERK,p38 MAPK,ROS	99%+
Fasudil HCl		✔		Rho,PKA	98%
ML-9		✔		MLCK,Akt	99%+
Flunarizine 2HCl		+ Calcium channel, Ki: 68 nM			95%
Lomerizine 2HCl		✔			98%
Efonidipine		✔			98%
Levamlodipine		✔			97%
Nisoldipine		++ L-type Cav1.2, IC50: 10 nM			97%
Isradipine		✔			98%
Lacidipine		✔			98%
Lercanidipine		✔			98%
Loureirin B		✔		Potassium Channel	99%+
Tetracaine HCl		✔			98%
Manidipine		+++ Calcium channel, IC50: 2.6 nM			98%
Manidipine Dihydrochlorid		+++ Calcium channel, IC50: 2.6 nM			98%
Nicardipine		✔			98%
Wilforgine		✔			98+%
Econazole		✔			99%+
Ginsenoside Rd		✔		NF-κB	98%
Fendiline HCl		✔			98+%
Mesaconitine		✔			98%
Tetrandrine		✔			95%
Nifedipine		✔			95%
Nilvadipine		++++ Calcium channel, IC50: 0.03 nM			98%
Barnidipine		++++ [³H]nitrendipine, Ki: 0.21 nM			95+%
Azelnidipine		✔			97%
Levetiracetam		✔			98%
Nimodipine		✔			95%
Benidipine HCl		✔			98%
Pinaverium bromide		✔			98%
Pranidipine		✔			98%
NP118809		+ L-type calcium channel, IC50: 12.2 μM N-type Ca2+ channel, IC50: 0.11 μM			98%
Amlodipine Besylate		+++ Calcium channel, IC50: 1.9 nM			97%
Cilnidipine		✔			98%
Cinepazide Maleate		✔			98%
Terfenadine		✔			98%
YM-58483		✔			99%+
Ranolazine		✔			98%
Praeruptorin A		✔		p38 MAPK,Akt	98%
Ranolazine 2HCl		✔			98%
Felodipine		++++ L-type calcium channel, IC50: 0.15 nM			98%
PD173212		+++ N-type Ca2+ channel, IC50: 36 nM			98%
Levamlodipine besylate		✔			97%
Carboxyamidotriazole Orotate		✔			98%
IGS-1.76		✔			98+%
WH-4-023		++++ Cav 2.2, IC50: 0.001 μM	++++ Cav 2.2, IC50: 0.001 μM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Verapamil HCl 生物活性

靶点

Calcium Channel

描述

Verapamil hydrochloride, a prototype calcium antagonist, is now marketed in the United States for the acute treatment of supraventricular tachyarrhythmias and for chronic management of vasospastic and chronic stable angina. It inhibits the slow inward channel in in the heart and blocks calcium influx in smooth muscle^[3]. Verapamil (hydrochloride) is an L-type calcium channel antagonist. The combination of Bortezomib and Verapamil (70 µM) markedly declines the viability of the JK-6L, RPMI 8226, and ARH-77 cell lines after 16 hours of culture^[4]. The enzyme hydrolase activity of recombinant human carboxylesterase (CES2) is substantially inhibited by Verapamil with Ki of 3.84±0.99μM^[5]. Verapamil (1 mg/kg) significantly decreases the incidence of ventricular arrhythmias including premature ventricular contractions (PVC), ventricular tachycardia (VT) and ventricular fibrillation (VF) for 45-min coronary artery occlusion. Verapamil may confer an anti-arrhythmic effect via calcium influx inhibition, inhibition of oxygen consumption and accompanied by preservation of Cx43 protein^[6]. Combined fractional CO2 laser and topical 5-FU (5-fluorouracil) or verapamil hydrochloride offer a safe therapy for HTSs (hypertrophic scars) and keloids^[7].

Verapamil HCl 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A2780 cells		Function assay		Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=4.57088 μM	18678495
Caco-2 cells		Function assay		Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=20 μM	17064079
CCRF-CEM cells	5 μM	Function assay		The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin, ED50=0.045 μM	7629817
CHO cells		Function assay		Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.14125 μM	18448342

Verapamil HCl 参考文献

[1]Yanjiao X, Chengliang Z, et al. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468-74.

[2]Meister S, Frey B, et al. Calcium channel blocker verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myeloma cells. Neoplasia. 2010 Jul;12(7):550-61.

[3]Baky SH, Singh BN. Verapamil hydrochloride: pharmacological properties and role in cardiovascular therapeutics. Pharmacotherapy. 1982;2(6):328‐353

[4]Meister S, Frey B, Lang VR, et al. Calcium channel blocker verapamil enhances endoplasmic reticulum stress and cell death induced by proteasome inhibition in myeloma cells. Neoplasia. 2010;12(7):550‐561

[5]Yanjiao X, Chengliang Z, Xiping L, Tao W, Xiuhua R, Dong L. Evaluation of the inhibitory effects of antihypertensive drugs on human carboxylesterase in vitro. Drug Metab Pharmacokinet. 2013;28(6):468‐474

[6]Zhou P, Zhang SM, Wang QL, Wu Q, Chen M, Pei JM. Anti-arrhythmic effect of verapamil is accompanied by preservation of cx43 protein in rat heart. PLoS One. 2013;8(8):e71567. Published 2013 Aug 12

[7]Sabry HH, Abdel Rahman SH, Hussein MS, Sanad RR, Abd El Azez TA. The Efficacy of Combining Fractional Carbon Dioxide Laser With Verapamil Hydrochloride or 5-Fluorouracil in the Treatment of Hypertrophic Scars and Keloids: A Clinical and Immunohistochemical Study. Dermatol Surg. 2019;45(4):536‐546

Verapamil HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.18mL

2.04mL

1.02mL

20.36mL

4.07mL

2.04mL

Verapamil HCl 技术信息

CAS号	152-11-4
分子式	C₂₇H₃₉ClN₂O₄
分子量	491.063

别名	CP-16533-1 hydrochloride;Verapamil (hydrochloride);NSC 657799;NSC 272366;(±)-Verapamil;CP-16533-1;Verapamil HCl;(±)-Verapamil hydrochloride
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 30 mg/mL(61.09 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 50 mg/mL(101.82 mM)，配合低频超声助溶

动物实验配方

细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源

A2780 cells		Function assay		Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=4.57088 μM	18678495
Caco-2 cells		Function assay		Inhibition of Pgp measured as inhibition of [3H]vinblastine basolateral to apical transport in Caco-2 cells, EC50=20 μM	17064079
CCRF-CEM cells	5 μM	Function assay		The effective dose was measured against P-glycoprotein expressing CCRF-CEM cells in the presence of 5 uM daunomycin, ED50=0.045 μM	7629817
CHO cells		Function assay		Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=0.14125 μM	18448342
hamster BHK21 cells		Cytotoxic assay	96 h	Cytotoxicity against hamster BHK21 cells expressing MRP1 after 96 hrs by MTT assay, IC50=10.6 μM	20691599
HCT116/VM46 cell	1 μM	Function assay		Effect on vinblastine IC50 against MDR human carcinoma HCT116/VM46 cell line at a dose of 1 uM concentration, IC50=0.004 μM	12729663
human 2008 cells		Function assay		Inhibition of human MRP1 in human 2008 cells, IC50=9.66 μM	18707884
human CEM/VLB500 cells		Function assay	3 days	Reversal of P-gp-mediated multidrug resistance to vinblastine in human CEM/VLB500 cells after 3 days by resazurin assay, EC50=1.041 μM	17399990
human H460 cells	50 μM	Function assay	72 h	Potentiation of erlotinib-induced cytotoxicity against human H460 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=10.3 μM	25215856
human K562/DOX cells		Function assay		Modulatory activity at P-gp in human K562/DOX cells assessed as increase in nuclear concentration of pirarubicin by spectrofluorometric assay, IC50=1.6 μM	25282263
human KB/VCR cells	25 μM	Cytotoxic assay	72 h	Cytotoxicity against human KB/VCR cells assessed as vincristine IC50 at 25 uM after 72 hrs by SRB method, IC50=0.02 μM	25597010
human KB/VCR cells		Function assay	72 h	Inhibition of p-gp in human KB/VCR cells assessed as potentiation of 100 nM docetaxel-induced cytotoxicity after 72 hrs by MTT assay, EC50=1.253 μM	23683834
human KB31 cells		Cytotoxic assay	48 h	Cytotoxicity against human KB31 cells after 48 hrs by SRB method, IC50=45.2 μM	10346948
human KBV1 cells		Cytotoxic assay	48 h	Cytotoxicity against vinblastine resistant human KBV1 cells after 48 hrs in presence of 100 nM vinblastine by SRB method, IC50=1.6 μM	10346948
human KBV20C cells		Cytotoxic assay		Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of paclitaxel by MTS assay, IC50=0.01 μM	18295490
human KBV20C cells		Cytotoxic assay		Cytotoxicity against multidrug resistant P-gp expressing human KBV20C cells assessed as cell viability in presence of vincristine by MTS assay, IC50=0.2 μM	18295490
human LCC6MDR cells		Function assay	5 days	Reversal of P-gp-mediated doxorubicin-resistance in human LCC6MDR cells after 5 days by MTS assay, EC50=0.245 μM	22320402
human MCF7/ADR cells	10 μM	Function assay	48 h	Inhibition of P-gp in human MCF7/ADR cells assessed as reversal of multidrug resistance at 10 uM by measuring EC50 for adriamycin-induced cytotoxicity after 48 hrs by SRB colorimetric assay, EC50=4.89 μM	25856545
human NCI-H292 cells	50 μM	Function assay	72 h	Potentiation of erlotinib-induced cytotoxicity against human NCI-H292 cells assessed as erlotinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=1.2 μM	25215856
K562 cells	3 μM	Function assay	72 h	Modulatory activity at P-gp assessed as doxorubicin IC50 in human K562 cells at 3 uM after 72 hrs by MTT assay (Rvb doxorubicin alone IC50 = 0.023 +/- 0.004 uM), IC50=0.029 μM	25282263
KB cells		Function assay	72 h	Inhibitory activity against KB cell line after 72 h of drug exposure, IC50=19.6 μM	15481991
KB-3-1 cells	5 μM	Function assay	68 h	Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-3-1 cells at 5 uM after 68 hrs by MTT assay, IC50=0.0047 μM	17488128
KB-C2 cells	5 μM	Function assay	68 h	Reversal of P-gp-mediated multidrug resistance to Cytotoxicity of colchicine against human KB-C2 cells at 5 uM after 68 hrs by MTT assay, IC50=0.1 μM	17488128
MCF7 cells		Function assay		Inhibition of human ERG in MCF7 cells, IC50=0.14454 μM	19110341
MDA435/LCC6 cells		Function assay		Reversal of vinblastine resistance in multidrug resistant MDA435/LCC6 cells by MTS assay, IC50=0.00025 μM	17154505
MDCK cells		Function assay	30 mins	Inhibition of human MDR1 expressed in MDCK cells assessed as calcein AM accumulation after 30 mins by fluorescence assay, IC50=0.5 μM	22112208
MDCK2 cells		Function assay	20 mins	Enhancement of calcein-AM uptake in MDCK2 cells over expressing MDR1 after 20 mins, EC50=5.1 μM	18849167
NCI-H292 cells	50 μM	Function assay	72 h	Potentiation of gefitinib-induced cytotoxicity against human NCI-H292 cells assessed as gefitinib IC50 at 50 uM after 72 hrs by SRB assay, IC50=0.18 μM	25215856
rat A7R5 cells		Function assay	15 mins	Antagonist activity at calcium channel in rat A7R5 cells assessed as inhibition of Cacl2/KCl-induced increase in intracellular Ca2+ incubated for 15 mins prior to Cacl2/KCl challenge by fluorescence assay, IC50=0.3 μM	25311564

盐酸维拉帕米 /Verapamil HCl {[allProObj[0].p_purity_real_show]}

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Verapamil HCl 质控信息

Verapamil HCl 生物活性

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Verapamil HCl 参考文献

Verapamil HCl 实验方案

Verapamil HCl 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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