DIDS sodium salt
(Synonyms: 4,4'-二异硫氰酸基-2,2'-二苯乙烯磺酸二钠[蛋白质改性试剂],MDL101114ZA) 目录号 : GC14830
DIDS 是一种阴离子转运抑制剂，可抑制 ClC-Ka 氯离子通道，IC50 为 100 μM 和细菌 ClC-ec1Cl-/H+ 交换器，IC50 约为 300 μM。
Cas No.:67483-13-0
Sample solution is provided at 25 µL, 10mM.
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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.
DIDS 是一种阴离子转运抑制剂,可抑制 ClC-Ka 氯离子通道,IC50 为 100 μM 和细菌 ClC-ec1Cl-/H+ 交换器,IC50 约为 300 μM。 [1]
氯离子通道是一个由大约13个亚群组成的超家族,在生理学上发挥着多种功能。人类基因组包含九种 CLC 蛋白,它们具有多种生理功能,并可能构成治疗高血压、骨质疏松症以及胃肠道和肾脏疾病的新型药物靶点。 [1]
采用穿孔补片技术研究了DIDS对兔门静脉肌肉细胞中钙激活氯化物电流[ICl(ca)]的影响。因此,DIDS 以浓度依赖性方式降低了自发瞬态内向电流 (STIC) 的振幅,STIC 的 IC50 值为 2.1 x 10-4 M。此外,研究了DIDS对大脑动脉平滑肌细胞收缩的作用。 DIDS 显示出对压力收缩动脉的血管扩张作用,IC50 为 69 ±； 14 &亩;M. [2, 3]
体内研究显示单独使用DIDS可增加42.5℃或43.5℃热疗抑制肿瘤生长的效果。当 DIDS 与阿米洛利联合使用时,热敏化作用更大。 43.5 ℃ 的热疗可导致肿瘤生长延迟 4 天,而热疗和 25 mg/kg DIDS 治疗将延迟延长至约 6 天。作为证据,细胞存活的体内-体外切除试验表明 DIDS 增强了热诱导的肿瘤细胞死亡。 [4]
| Cell experiment [1]: | |
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Cell lines |
DRG(dorsal root ganglion) neurons extracted from the spinal levels of 6- to 8-week-old Sprague-Dawley rats |
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Preparation method |
Soluble in DMSO > 10mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1, 1, 3, 10, 100μm for 2min; simultaneous detection from adding first drop |
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Applications |
In DRG neurons, although DIDS did not induce the activation of TRPV1(Transient receptor potential vanilloid type 1) per se but drastically increased the TRPV1 currents induced by either capsaicin or low pH. DIDS could modify TRPV1 channel function in an agonist-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
4–5 day old newborn healthy Sprague-Dawley rats (both males and females) |
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Dosage form |
5 mg/kg, intraperitoneal injection |
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Application |
DIDS significantly reduced the elevated mRNA levels and protein expression of chloride channel 2 (ClC-2) in neonatal rats induced by ischemia-hypoxia. DIDS application significantly decreased the concentrations of reactive oxygen species (ROS); and the mRNA levels of inducible nitric oxide synthase (iNOS) and tumor necrosis factor-alpha(TNF-α) in neonatal rats with hypoxic-ischemic damage. The elevated number of caspase-3 and neural/glial antigen 2 (NG-2) double-labeled positive cells was attenuated by DIDS after ischemia anoxic injury. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 67483-13-0 | SDF | |
| 别名 | 4,4'-二异硫氰酸基-2,2'-二苯乙烯磺酸二钠[蛋白质改性试剂],MDL101114ZA | ||
| 化学名 | sodium (E)-6,6'-(ethene-1,2-diyl)bis(3-isothiocyanatobenzenesulfonate) | ||
| Canonical SMILES | S=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+] | ||
| 分子式 | C16H8N2Na2O6S4 | 分子量 | 498.48 |
| 溶解度 | 50mg/ml in DMSO (ultrasonic and warming and heat to 60°C); 30mg/ml in Water ( Need ultrasonic) | 储存条件 | Store at -20°C, sealed storage, away from moisture |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0061 mL | 10.0305 mL | 20.061 mL |
| 5 mM | 0.4012 mL | 2.0061 mL | 4.0122 mL |
| 10 mM | 0.2006 mL | 1.003 mL | 2.0061 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet