DCPIB 是一种选择性、可逆、有效的体积调节性阴离子通道 (VRAC) 抑制剂。DCPIB 能够电压依赖性地激活钾离子通道TREK1和TRAAK，抑制TRESK，TASK1和TASK3(IC50值分别为 0.14，0.95，50.72 μM)。DCPIB 也可抑制肿胀激活的氯电流 (ICl,swell)，IC50值为 4.1 μM。DCPIB 是研究 K2P 通道的结构功能的工具。
| 生物活性 | DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channelsTREK1andTRAAK, and inhibitsTRESK,TASK1andTASK3(IC50s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with anIC50of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels[1][2]. |
| IC50& Target | IC50：0.14 μM (TRESK), 0.95 μM (TASK1), 50.72 μM (TASK3)[1], 4.1 μM (ICl,swell, CPAE cells)[2] |
体外研究
(In Vitro) | DCPIB (10 μM) activates TREK1 and enhances TRAAK currents in COS-7 cells[1].
DCPIB (10 μM) prominently and reversibly suppresses TRESK currents in COS-7 cells, with an IC50of 0.14 μM[1].
DCPIB (10 μM) displays selectivity for ICl,swelland has no significant inhibitory effects on ICl,Cain CPAE cells[2].
DCPIB (10 μM, 5 min) has no effect on attenuate subsequent swelling in cardiomyocytes[2].
DCPIB (10 μM, 3 h) inhibits LPS-induced MAPK activation in BV2 cells[3].
Immunofluorescence[3] | Cell Line: | BV2 cells | | Concentration: | 10 μM | | Incubation Time: | 3 h | | Result: | Significantly decreased Ki67 positive staining microglia and pro-inflammatory cytokine (TNF-α, IL-1β) secretion. |
Western Blot Analysis[3] | Cell Line: | BV2 cells | | Concentration: | 10 μM | | Incubation Time: | 3 h | | Result: | Inhibited migratory potential of transient OGD (Oxygen-glucose deprivation) exposed BV2 cells. |
|
体内研究
(In Vivo) | LDN-212854 (intracerebroventricular infusion, 1 mM, 10 μL) suppresses microglial activation and ameliorates neuronal damage in rMCAO rats[3].
| Animal Model: | Reversible middle cerebral artery occlusion (rMCAO) model[3] | | Dosage: | 1 mM, 10 μL | | Administration: | Administered manually for 20s by intracerebroventricular infusion | | Result: | Diminished Pyramidal neurons injury induced by rMCAO in the CA1 region. |
|
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(233.99 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3399 mL | 11.6997 mL | 23.3995 mL | | 5 mM | 0.4680 mL | 2.3399 mL | 4.6799 mL | | 10 mM | 0.2340 mL | 1.1700 mL | 2.3399 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.87 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.87 mM); Clear solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.87 mM) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
