切换导航

DIDS

现货
Catalog No.
B7675
阴离子运输抑制剂
组合的产品项目
规格价格库存 数量
50mg
¥ 770.00
Ship with 7 days

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

DIDS is an anion transport inhibitor, which inhibits the ClC-Ka chloride channel with an IC50 of 100 μM and the bacterial ClC-ec1Cl-/H+ exchanger with an IC50 of ~300 μM. [1]
Chloride channels are a superfamily consisting of approximately 13 subgroups and display a variety of functions in physiology. The human genome contains nine CLC proteins, which serve various physiological functions and potentially constitute novel exciting drug targets for the treatment of hypertension, osteoporosis, and gastrointestinal and renal disorders. [1]
DIDS’s effect on the calcium-activated chloride current [ICl (ca)] in muscle cells from the rabbit portal vein was studied with the perforated patch technique. Consequently, DIDS reduced the amplitude of spontaneous transient inward currents (STICs) in a concentration-dependent manner with an IC50 value of 2.1 x 10-4 M for STICs. Moreover, DIDS was investigated for its action on contraction of cerebral artery smooth muscle cells. DIDS showed a vasodilator effect on pressure-constricted arteries with IC50 of 69 ± 14 μM. [2, 3]
In vivo study showed DIDS alone increased the effect of hyperthermia at 42.5 ℃ or 43.5 ℃ to suppress tumor growth. The thermosensitization was greater when DIDS was combined with amiloride. Hyperthermia at 43.5 ℃ could result in a tumor growth delay for 4 days, while hyperthermia and treatment of 25 mg/kg DIDS prolonged the delay to approximately 6 days. As a proof, in vivo-in vitro excision assays for cell survival illustrated that DIDS enhanced the heat-induced tumor cell death.  [4]
References:
[1] Wulff, Heike. "New light on the “Old” chloride channel blocker DIDS." ACS chemical biology 3.7 (2008): 399-401.
[2] Hogg, R. C., Q. Wang, and W. A. Large. "Effects of Cl channel blockers on Ca‐activated chloride and potassium currents in smooth muscle cells from rabbit portal vein." British journal of pharmacology 111.4 (1994): 1333-1341.
[3] Nelson, Mark T., et al. "Chloride channel blockers inhibit myogenic tone in rat cerebral arteries." The Journal of Physiology 502.2 (1997): 259-264.
[4] Lyons, John C., Brian D. Ross, and Chang W. Song. "Enhancement of hyperthermia effect in vivo by amiloride and DIDS." International Journal of Radiation Oncology* Biology* Physics 25.1 (1993): 95-103.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt498.48
Cas No.67483-13-0
FormulaC16H8N2Na2O6S4
Solubility<3.72mg/mL in DMSO,<3.33mg/mL in Ethanol,<3.03mg/ml in H2O
Chemical Namesodium (E)-6,6'-(ethene-1,2-diyl)bis(3-isothiocyanatobenzenesulfonate)
SDFDownload SDF
Canonical SMILESS=C=NC1=CC=C(/C=C/C(C(S([O-])(=O)=O)=C2)=CC=C2N=C=S)C(S([O-])(=O)=O)=C1.[Na+].[Na+]
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

来源于6-8周龄Sprague-Dawley大鼠的DRG(背根神经节)神经元细胞

溶解方法

在DMSO中的溶解度>10mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月

反应时间

0.1, 1, 3, 10, 100μm作用2min,加入第一滴药物开始同时观察

应用

在DGR神经元中,尽管DIDS并没有诱导TRPV1(瞬时受体电位香草酸亚型1型)自身的活化,但是显著提高了辣椒素或低pH诱导的TRPV1电流。DIDS可以以激动剂依赖的方式改变TRPV1通道功能。

动物实验[2]:

动物模型

雄性和雌性的4-5日龄新生健康Sprague-Dawley大鼠

剂量

5 mg/kg,腹腔注射

应用

在新生大鼠中,DIDS能够显著降低局部缺血诱导的mRNA水平的提高和ClC-2(氯化物通道2)的蛋白表达。在局部缺氧缺血伤害的新生大鼠中,DIDS的应用能够显著降低ROS(活性氧)的水平,iNOS(诱导型一氧化氮合酶)和TNF-α(肿瘤坏死因子α)的mRNA水平。在局部缺血缺氧损伤后的大鼠中,DIDS的使用减弱了caspase-3和NG-2(神经/神经胶质抗原2)双重标记阳性的细胞数的增加。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Zhang X1, Du XN, et al, Agonist-dependent potentiation of vanilloid receptor transient receptor potential vanilloid type 1 function by stilbene derivatives. Mol Pharmacol. 2012 May;81(5):689-700. doi: 10.1124/mol.111.076000. Epub 2012 Feb 10.

[2]. Zhao B1, Quan H2, 4,4'-Diisothiocyanostilbene-2,2'-disulfonic Acid (DIDS) Ameliorates Ischemia-Hypoxia-Induced White Matter Damage in Neonatal Rats through Inhibition of the Voltage-Gated Chloride Channel ClC-2. Int J Mol Sci. 2015 May 7;16(5):10457-69. doi: 10.3390/ijms160510457.

质量控制

化学结构

DIDS