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DCPIB {[allProObj[0].p_purity_real_show]}

货号:A1176584

DCPIB是一种体积调节性阴离子通道(VRAC)抑制剂,能有效抑制细胞的钠钾通道和氯电流。它在细胞肿胀和离子通道研究中具有应用潜力。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
DCPIB 化学结构 CAS号:82749-70-0
DCPIB 化学结构
CAS号:82749-70-0
DCPIB 3D分子结构
CAS号:82749-70-0
DCPIB 化学结构 CAS号:82749-70-0
DCPIB 3D分子结构 CAS号:82749-70-0
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DCPIB 纯度/质量文件 产品仅供科研

货号:A1176584 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Potassium Channel 其他靶点 纯度
Tolbutamide 98%
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SUR2B, IC50: 7.3 nM

SUR1, IC50: 5.4 nM

97%
Dronedarone HCl 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

99%
TRAM-34 +++

IKCa1 (KCa3.1), Kd: 20 nM

98%
Glibenclamide 98%
Amiodarone HCl 97%
Gliclazide ++

Potassium channel, IC50: 184 nM

98%
Repaglinide 98%
Dofetilide 98%
Nateglinide 99%
Quinine HCl dihydrate 98%
ML133 HCl +

Kir2.1, IC50: 290 nM

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。

DCPIB 生物活性

描述 DCPIB is a selective, reversible and potent inhibitor of VRAC. DCPIB voltage-dependently activates the potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1, and TASK3 (IC50 values of 0.14, 0.95, and 50.72 μM, respectively). DCPIB is also a selective and swelling-induced blocker of chloride current with an IC50 value of 4.1 μM. DCPIB is an effective tool to study the structure-function of K2P channels. DCPIB at a concentration of 10 μM activates TREK1 and enhances TRAAK currents in COS-7 cells[1][2]. At the same concentration, DCPIB significantly and reversibly inhibited TRESK current in COS-7 cells with an IC50 of 0.14 μM[1]. While acting for 3 hours, DCPIB inhibited LPS-induced MAPK activation in BV2 cells[3].

DCPIB 细胞实验

Cell Line
Concentration Treated Time Description References
HEK-293 cells HEK-293 cells SN-401 inhibited ICl,SWELL currents with an IC50 of 3.9 µM Nat Commun. 2022 Feb 10;13(1):784.
HK-2 cells HK-2 cells Inhibited TGFβ1-induced chloride currents and GSH conductance Cell Death Dis. 2019 Dec 5;10(12):925.
cardiomyocytes cardiomyocytes alleviated tunicamycin-induced ER stress and apoptosis Cell Death Dis. 2014 Nov 20;5(11):e1528.
human umbilical vein endothelial cells (HUVECs) human umbilical vein endothelial cells (HUVECs) SN-401 increased eNOS phosphorylation (Ser1177), and this effect was abrogated by SWELL1 knockdown in HUVECs Nat Commun. 2022 Feb 10;13(1):784.
3T3-F442A adipocytes 3T3-F442A adipocytes SN-401 increased SWELL1 protein expression 1.5-fold and enhanced insulin-stimulated pAKT2 and pAS160 signaling Nat Commun. 2022 Feb 10;13(1):784.
3T3-F442A preadipocytes 3T3-F442A preadipocytes SN-401 increased SWELL1 protein expression threefold and enhanced insulin-stimulated pAKT2 signaling Nat Commun. 2022 Feb 10;13(1):784.
HL-1 cardiomyocytes HL-1 cardiomyocytes Inhibited ET-1-induced volume-sensitive Cl⁻ current (ICl,swell) Cardiovasc Res. 2010 Oct 1;88(1):93-100.
rabbit ventricular myocytes rabbit ventricular myocytes Inhibited ET-1-induced volume-sensitive Cl⁻ current (ICl,swell) Cardiovasc Res. 2010 Oct 1;88(1):93-100.
rabbit atrial myocytes rabbit atrial myocytes Inhibited ET-1-induced volume-sensitive Cl⁻ current (ICl,swell) Cardiovasc Res. 2010 Oct 1;88(1):93-100.
rabbit ventricular myocytes rabbit ventricular myocytes DCPIB inhibited the volume-sensitive chloride current activated by C2-Cer and bacterial SMase Cardiovasc Res. 2010 Apr 1;86(1):55-62.
Hippocampal slices Hippocampal slices Inhibited VRAC channels, preventing oxidative stress-induced taurine efflux J Biomed Sci. 2010 Aug 24;17 Suppl 1(Suppl 1):S10.
HEK293-WT cells HEK293-WT cells Inhibited LRRC8/VRAC-dependent GSH conductance and marked decrease in intracellular GSH content under hypotonic conditions Cell Death Dis. 2019 Dec 5;10(12):925.
cardiomyocytes cardiomyocytes inhibited tunicamycin-induced activation of VSOR Cl− currents Cell Death Dis. 2014 Nov 20;5(11):e1528.
Vascular smooth muscle cells (VSMC) Vascular smooth muscle cells (VSMC) DCPIB significantly inhibited TNFα-induced NF-κB activation Free Radic Biol Med. 2016 Dec;101:413-423.
HEK293 cells HEK293 cells DCPIB inhibited NF-κB activation in a concentration-dependent manner Free Radic Biol Med. 2016 Dec;101:413-423.
PC12 cells PC12 cells To evaluate the inhibitory effect of DCPIB on hypotonic-induced changes in intracellular chloride concentration, results showed DCPIB blocked hypotonic-induced decrease in [Cl–]i Acta Pharmacol Sin. 2013 Jan;34(1):113-8.
PC12 cells PC12 cells To evaluate the inhibitory effect of DCPIB on OGD-induced cell death, results showed DCPIB significantly reduced OGD-induced cell death Acta Pharmacol Sin. 2013 Jan;34(1):113-8.
primary cultured cortical neurons primary cultured cortical neurons To investigate the inhibitory effect of DCPIB on the swelling-induced chloride current (ICl,swell). Results showed that DCPIB completely inhibited the ICl,swell activated by a 30% hypotonic solution. Acta Pharmacol Sin. 2018 May;39(5):858-865.
COS-7 cells COS-7 cells Test the modulatory effect of DCPIB on TWIK2 channel, results showed no significant inhibition on TWIK2 channel Acta Pharmacol Sin. 2022 Apr;43(4):992-1000.

DCPIB 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Obese, HFD-fed T2D model and polygenic-T2D KKAy mouse model Intraperitoneal injection 5 mg/kg Once daily for 4–10 days SN-401 increased SWELL1 expression in adipose tissue (twofold in HFD mice, threefold in KKAy mice), improved fasting blood glucose, glucose tolerance, and insulin tolerance, increased insulin sensitivity, and reduced hepatic steatosis and hepatocyte damage Nat Commun. 2022 Feb 10;13(1):784.
CD1 mice Neonatal hypoxic-ischemic injury model Intraperitoneal injection 10 mg/kg Single dose, 20 minutes before ischemia To evaluate the neuroprotective effect of DCPIB on neonatal hypoxic-ischemic injury, results showed DCPIB significantly reduced brain infarct volume and improved neurobehavioral outcomes Acta Pharmacol Sin. 2013 Jan;34(1):113-8.
CD1 mice Neonatal mouse hypoxic-ischemic brain injury model Intraperitoneal injection 10 mg/kg Single dose, approximately 20 minutes before ischemia To evaluate the protective effects of DCPIB on neonatal hypoxic-ischemic brain injury. Results showed that pretreatment with DCPIB significantly reduced brain damage (assessed by TTC staining, Nissl staining, and whole brain imaging) and improved sensorimotor and vestibular recovery outcomes in neurobehavioral tests (i.e., geotaxis reflex and cliff avoidance reflex). Acta Pharmacol Sin. 2018 May;39(5):858-865.

DCPIB 参考文献

[1]Lv J, et al. DCPIB, an Inhibitor of Volume-Regulated Anion Channels, Distinctly Modulates K2P Channels. ACS Chem Neurosci. 2019 Apr 17.

[2]Decher N, et al. DCPIB is a novel selective blocker of I(Cl,swell) and prevents swelling-induced shortening of guinea-pig atrial action potential duration. Br J Pharmacol. 2001 Dec;134(7):1467-79.

[3]Han Q, Liu S, Li Z, Hu F, Zhang Q, Zhou M, Chen J, Lei T, Zhang H. DCPIB, a potent volume-regulated anion channel antagonist, attenuates microglia-mediated inflammatory response and neuronal injury following focal cerebral ischemia. Brain Res. 2014 Jan 13;1542:176-85. doi: 10.1016/j.brainres.2013.10.026. Epub 2013 Nov 1. PMID: 24189520.

DCPIB 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.40mL

4.68mL

2.34mL

DCPIB 技术信息

CAS号82749-70-0
分子式C22H28Cl2O4
分子量 427.36
SMILES Code O=C1C2=C(Cl)C(Cl)=C(OCCCC(O)=O)C=C2CC(C3CCCC3)1CCCC
MDL No. MFCD07783995
别名
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 105 mg/mL(245.69 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

请根据您的动物给药指南选择适当的溶解方案。
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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