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| 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 | ✔ | 99% | |||||||||||||||||
| 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 HCl | ✔ | 95% | |||||||||||||||||
| Nitrendipine |
+
Calcium channel, IC50: 95 nM |
98% | |||||||||||||||||
| Efonidipine HCl monoethanolate | ✔ | 98% | |||||||||||||||||
| Cinnarizine | ✔ | 98% | |||||||||||||||||
| SEA0400 |
++
NCX, IC50: 33 nM |
ERK,ROS,p38 MAPK | 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 | ✔ | 98% | |||||||||||||||||
| Nisoldipine |
++
L-type Cav1.2, IC50: 10 nM |
97% | |||||||||||||||||
| Isradipine | ✔ | 98% | |||||||||||||||||
| Lacidipine | ✔ | 98% | |||||||||||||||||
| Lercanidipine | ✔ | 99% | |||||||||||||||||
| Loureirin B | ✔ | Potassium Channel | 99%+ | ||||||||||||||||
| Tetracaine HCl | ✔ | 98% | |||||||||||||||||
| Manidipine |
+++
Calcium channel, IC50: 2.6 nM |
99% | |||||||||||||||||
| Manidipine Dihydrochlorid |
+++
Calcium channel, IC50: 2.6 nM |
98% | |||||||||||||||||
| Nicardipine | ✔ | 99% | |||||||||||||||||
| Wilforgine | ✔ | 98+% | |||||||||||||||||
| Econazole | ✔ | 99%+ | |||||||||||||||||
| Ginsenoside Rd | ✔ | NF-κB | 98% | ||||||||||||||||
| Fendiline HCl | ✔ | 98+% | |||||||||||||||||
| Mesaconitine | ✔ | 98% | |||||||||||||||||
| Tetrandrine | ✔ | 95% | |||||||||||||||||
| Nifedipine | ✔ | 98% | |||||||||||||||||
| Nilvadipine |
++++
Calcium channel, IC50: 0.03 nM |
95% | |||||||||||||||||
| Barnidipine |
++++
[3H]nitrendipine, Ki: 0.21 nM |
95+% | |||||||||||||||||
| Azelnidipine | ✔ | 97% | |||||||||||||||||
| Levetiracetam | ✔ | 98% | |||||||||||||||||
| Nimodipine | ✔ | 95% | |||||||||||||||||
| Benidipine HCl | ✔ | 98% | |||||||||||||||||
| Pinaverium bromide | ✔ | 98% | |||||||||||||||||
| Pranidipine | ✔ | 99% | |||||||||||||||||
| NP118809 |
+
L-type calcium channel, IC50: 12.2 μM N-type Ca2+ channel, IC50: 0.11 μM |
95% | |||||||||||||||||
| Amlodipine Besylate |
+++
Calcium channel, IC50: 1.9 nM |
97% | |||||||||||||||||
| Cilnidipine | ✔ | 99% | |||||||||||||||||
| Cinepazide Maleate | ✔ | 99% (HPLC) | |||||||||||||||||
| Terfenadine | ✔ | 98% | |||||||||||||||||
| YM-58483 | ✔ | 99%+ | |||||||||||||||||
| Amiloride HCl | ✔ | 98% | |||||||||||||||||
| Ranolazine | ✔ | 98% | |||||||||||||||||
| Praeruptorin A | ✔ | Akt,p38 MAPK | 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Pinaverium bromide acts as a calcium channel blocker in helping to restore the normal contraction process of the bowel. |
| Concentration | Treated Time | Description | References | |
| Rat colonic smooth muscle cells | 0.1 – 10 µM | 20 minutes | To investigate the inhibitory effect of pinaverium on ACh or KCl-induced [Ca2+]i increment, results showed pinaverium inhibited [Ca2+]i increment in a dose-dependent manner. | World J Gastroenterol. 2003 Mar;9(3):557-61 |
| Human hepatocellular carcinoma cells HepG2 and Huh7 | <50 µM | 24 hours | Pinaverium bromide significantly inhibited cell viability at high concentrations (50 or 100 μM). | ACS Omega. 2023 Mar 6;8(10):9652-9661 |
| Staphylococcus aureus CHS101 isolate | 50 µM | 24 hours | Pinaverium bromide significantly inhibited the growth of planktonic cells and biofilm formation of S. aureus CHS101 isolate. | ACS Omega. 2023 Mar 6;8(10):9652-9661 |
| Rabbit jejunum longitudinal smooth muscle cells | 1-100 µM | 5 minutes | To study the inhibitory effect of pinaverium on voltage-dependent inward current, with an IC50 of 1.5 μM, similar to verapamil, diltiazem, and flunarizine. Occasionally, a potentiating effect on inward current was observed. | Br J Pharmacol. 1990 Feb;99(2):374-8 |
| Administration | Dosage | Frequency | Description | References | ||
| Male Wistar rats | Cold-restraint stress model | In vitro tissue bath | 100 nM - 30 µM | Single administration, at least 15 min equilibration for each concentration | To investigate the effect of pinaverium on stress-induced colonic smooth muscle contractility disorder, results showed pinaverium inhibited ACh or KCl-induced muscle contraction in a dose-dependent manner. | World J Gastroenterol. 2003 Mar;9(3):557-61 |
| Wistar rats | Diarrhoea model | Gavage | 13.5 mg/kg | Once daily for 7 consecutive days | To evaluate the protective effect of Pinaverium Bromide on diarrhoea rats, results showed that Pinaverium Bromide significantly improved diarrhoea symptoms. | Pharm Biol. 2021 Dec;59(1):1452-1463 |
| Rats | Rat isolated colon model | Organ bath administration | 3.4 μM (BaCl2 stimulation), 5.2μM (acetylcholine stimulation), 3.3μM (FK33-824 stimulation) | Single administration | To investigate the effect of Pinaverium bromide on the motility of rat isolated colon, results showed that it reduces calcium influx by inhibiting calcium channels, producing a spasmolytic effect, and its effect is 30 times weaker than verapamil | Br J Pharmacol. 1985 Sep;86(1):89-94 |
| Sprague-Dawley rats | Chronic visceral hypersensitivity model | Intragastric administration | 5 mg/mL | Once daily for 7 consecutive days | Pinaverium bromide significantly decreased abdominal withdrawal reflex scores in rats with chronic visceral hypersensitivity and significantly reduced P2X4 receptor immunoreactivity in the colon and spinal cord. | Neural Regen Res. 2013 Aug 5;8(22):2069-77 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01641224 | Irritable Bowel Syndrome | Not Applicable | Unknown | May 2014 | China, Jiangsu ... 展开 >> Second Jiangsu Provincial Hospital of Traditional Chinese Medicine affiliated to Nanjing University of Traditional Chinese Medicine Nanjing, Jiangsu, China, 210017 Jiangsu Provincial Hospital of Traditional Chinese Medicine affiliated to Nanjing University of Traditional Chinese Medicine Nanjing, Jiangsu, China, 210029 China Beijing Xuanwu Hospital of Traditional Chinese Medicine affiliated to Capital Medical University. Beijing, China, 100050 Shanghai First People's Hospital affiliated to Shanghai Tiao Tong University Shanghai, China, 200240 收起 << |
| NCT02330029 | Irritable Bowel Syndrome | Not Applicable | Unknown | May 2017 | China, Jiangsu ... 展开 >> Second Jiangsu Provincial Hospital of Traditional Chinese Medicine affiliated to Nanjing University of Traditional Chinese Medicine Nanjing, Jiangsu, China, 210017 Jiangsu Provincial Hospital of Traditional Chinese Medicine affiliated to Nanjing University of Traditional Chinese Medicine Nanjing, Jiangsu, China, 210029 China Beijing Xuanwu Hospital of Traditional Chinese Medicine affiliated to Capital Medical University. Beijing, China, 100050 Shanghai First People's Hospital affiliated to Shanghai Tiao Tong University Shanghai, China, 200240 收起 << |
| NCT01678781 | - | Completed | - | China ... 展开 >> Site reference ID/Investigator# 94519 Beijing, China, 100034 Site reference ID/Investigator# 95475 Guangzhou City, China, 510515 Site reference ID/Investigator# 94521 Guangzhou, China, 510080 Site reference ID/Investigator # 94518 Shanghai, China, 200127 Site reference ID/Investigator # 94517 Shanghai, China, 200433 Site reference ID/Investigator # 94516 Shanghai, China Site reference ID/Investigator # 94515 Wuhan, China, 430022 Egypt Site Reference ID/Investigator# 95908 Alexandria, Egypt Site reference ID/Investigator# 95900 Cairo, Egypt Site reference ID/Investigator# 95901 El Sharkya, Egypt Site reference ID/Investigator# 95902 Giza, Egypt Site reference ID/Investigator# 95903 Giza, Egypt Site Reference ID/Investigator# 95906 Port Said, Egypt Mexico Site reference ID/Investigaot# 94525 Guadalajara, Mexico, 49000 Site refernce ID/Investigator# 94527 Mexico City, Mexico, 54055 Site reference ID/Investigator# 94523 Tampico, Mexico, 89190 Poland Site reference ID/Investigator# 85314 Bialystok, Poland, 15-270 Site Reference ID/Investigator# 85297 Bialystok, Poland, 15-351 Site Reference ID/Investigator# 85298 Bydgoszcz, Poland, 85-079 Site Reference ID/Investigator# 85293 Katowice, Poland, 40-031 Site Reference ID/Investigator# 85296 Lodz, Poland, 91-473 Site reference ID/Investigator# 85313 Olsztyn, Poland, 10-501 Site Reference ID/Investigator# 85295 Poznan, Poland, 60-193 Site Reference ID/Investigator# 85294 Poznan, Poland, 60-539 收起 << | |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.69mL 0.34mL 0.17mL |
8.45mL 1.69mL 0.85mL |
16.91mL 3.38mL 1.69mL |
|
| CAS号 | 53251-94-8 |
| 分子式 | C26H41Br2NO4 |
| 分子量 | 591.42 |
| SMILES Code | CC1(C)C2CCC(CCOCC[N+]3(CC4=CC(OC)=C(OC)C=C4Br)CCOCC3)C1C2.[Br-] |
| MDL No. | MFCD01713435 |
| 别名 | Icosapentaenoic acid |
| 运输 | 蓝冰 |
| InChI Key | IKGXLCMLVINENI-UHFFFAOYSA-M |
| Pubchem ID | 40703 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, room temperature |
| 溶解方案 |
DMSO: 50 mg/mL(84.54 mM),配合低频超声助溶,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: 10 mg/mL(16.91 mM),配合低频超声,并水浴加热至45℃助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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