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DIDS sodium salt

Cat No.:V29674 Purity: ≥98%
DIDS sodium salt (MDL101114ZA) is a dual (bifunctional) inhibitor of ABCA1 and VDAC1.
DIDS sodium salt
DIDS sodium salt Chemical Structure CAS No.: 67483-13-0
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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50mg
100mg
250mg
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Other Forms of DIDS sodium salt:

  • DIDS
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Top Publications Citing lnvivochem Products
Product Description
DIDS sodium salt (MDL101114ZA) is a dual (bifunctional) inhibitor of ABCA1 and VDAC1.
DIDS sodium salt (CAS 67483-13-0), also known as 4,4'-Diisothiocyano-2,2'-stilbene disulfonic acid disodium salt, is a stilbene sulfonate that acts as an anion transport inhibitor. With a molecular formula of C₁₆H₈N₂Na₂O₆S₄ and a molecular weight of 500.50 g/mol, this compound is a dual ABCA1 and VDAC1 inhibitor. DIDS sodium salt inhibits Cl- uptake through plasma membrane-localized Cl- channels in order to study chloride transport. It also effectively inhibits various sodium-coupled bicarbonate transporters. The compound is a small molecule blocker/inhibitor of voltage-dependent anion channel 1 (VDAC1), inhibits apoptosis and VDAC oligomerization, and also inhibits RAD51-mediated homologous pairing and strand exchange reactions. It inhibits the ClC-Ka chloride channel and the bacterial ClC-ec1 Cl-/H+ exchanger with IC₅₀ of 100 μM and ~300 μM, respectively.
Biological Activity I Assay Protocols (From Reference)
Targets
DIDS sodium salt targets multiple ion channels and transporters. It inhibits anion transport, including Cl- uptake through plasma membrane-localized Cl- channels. It effectively inhibits various sodium-coupled bicarbonate transporters. The compound is a dual ABCA1 and VDAC1 inhibitor. As a VDAC1 inhibitor, it inhibits apoptosis and VDAC oligomerization. It also inhibits RAD51-mediated homologous pairing and strand exchange reactions. The compound inhibits the ClC-Ka chloride channel with an IC₅₀ of 100 μM and the bacterial ClC-ec1 Cl-/H+ exchanger with an IC₅₀ of ~300 μM. Its ability to inhibit multiple transport proteins makes it a valuable tool for studying ion transport and apoptosis.
ln Vitro
DIDS at doses lower than 400 μM has no clear deleterious effect on cell viability. DIDS pretreatment at 100 and 200 μM dosages decreased ALA-SDT-induced cell death, but the 50 μM dose showed no inhibitory impact. DIDS alone at a dose of 400 μM marginally reduced cell viability, but there was no statistically significant difference compared to untreated controls. DIDS (100 μM) pretreatment strongly reduces caspase-3 and caspase-9 activation [2].
In vitro studies have demonstrated that DIDS sodium salt is an effective inhibitor of anion transport. It inhibits Cl- uptake through plasma membrane-localized Cl- channels. It effectively inhibits various sodium-coupled bicarbonate transporters. The compound inhibits the ClC-Ka chloride channel with an IC₅₀ of 100 μM and the bacterial ClC-ec1 Cl-/H+ exchanger with an IC₅₀ of ~300 μM. As a VDAC1 inhibitor, it inhibits apoptosis and VDAC oligomerization. It also inhibits RAD51-mediated homologous pairing and strand exchange reactions.
ln Vivo
In vivo, DIDS sodium salt is used as a research tool to study ion transport and apoptosis. Its ability to inhibit VDAC1 and anion transport makes it valuable for studying mitochondrial function and cell death. However, DIDS sodium salt is not used as a therapeutic agent and is primarily a research reagent.
Enzyme Assay
In vitro non-cell enzyme assays for DIDS sodium salt typically involve measuring the inhibition of anion transport using membrane vesicles or liposomes. The compound is incubated with the vesicles and a radiolabeled anion (e.g., [³⁶Cl]Cl⁻), and the amount of radioactivity transported is measured. IC₅₀ values are calculated from dose-response curves. The inhibition of VDAC1 can be assessed using purified VDAC1 protein reconstituted into liposomes or planar lipid bilayers. These assays provide quantitative data on the compound's direct effects on its molecular targets.
Cell Assay
In vitro cell-based assays for DIDS sodium salt use various cell lines to study its effects on ion transport and apoptosis. Cells are treated with varying concentrations of the compound, and parameters such as chloride flux, intracellular pH, cell viability (MTT or CCK-8 assays), and apoptosis (Annexin V/PI staining) are assessed. The compound's effects on VDAC1 oligomerization are assessed by Western blotting using cross-linking agents. RAD51-mediated homologous recombination is assessed using reporter assays.
Animal Protocol
In vivo animal studies for DIDS sodium salt are limited, as the compound is primarily used as a research reagent. It may be used in animal models to study the role of VDAC1 or anion transport in disease, but specific in vivo studies are not extensively documented in the available literature.
ADME/Pharmacokinetics
DIDS sodium salt has a molecular weight of 500.50 g/mol and a molecular formula of C₁₆H₈N₂Na₂O₆S₄. It is also known as 4,4'-Diisothiocyano-2,2'-stilbene disulfonic acid disodium salt. The compound has a purity of ≥80%. It should be stored under appropriate conditions as recommended by the manufacturer. Detailed pharmacokinetic parameters are not applicable as the compound is not used as a therapeutic agent.
Toxicity/Toxicokinetics
The toxicity profile of DIDS sodium salt has not been comprehensively evaluated in published studies. As a research reagent, it is not intended for human therapeutic use. The compound's ability to inhibit ion transport and VDAC1 suggests that it may have significant biological effects that require careful evaluation. Standard laboratory safety precautions should be followed when handling the compound.
References

[1]. Inhibition of VDAC1 prevents Ca²⁺-mediated oxidative stress and apoptosis induced by 5-aminolevulinic acid mediated sonodynamic therapy in THP-1 macrophages. Apoptosis. 2014 Dec;19(12):1712-26.

[2]. Activation of soluble guanylyl cyclase prevents foam cell formation and atherosclerosis. Acta Physiol (Oxf). 2014 Apr;210(4):799-810.

Additional Infomation
Inhibit anion conduction, including inhibiting band 3-mediated anion transport.
DIDS sodium salt is a stilbene sulfonate that acts as an anion transport inhibitor. It is also known as 4,4'-Diisothiocyano-2,2'-stilbene disulfonic acid disodium salt. The compound is a dual ABCA1 and VDAC1 inhibitor. It inhibits Cl- uptake through plasma membrane-localized Cl- channels and effectively inhibits various sodium-coupled bicarbonate transporters. DIDS sodium salt inhibits VDAC1, apoptosis, and VDAC oligomerization, and also inhibits RAD51-mediated homologous pairing and strand exchange reactions. Not approved for therapeutic use; intended for research purposes only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H8N2NA2O6S4
Molecular Weight
498.4841
Exact Mass
497.906
CAS #
67483-13-0
Related CAS #
DIDS;53005-05-3
PubChem CID
5702690
Appearance
Light yellow to yellow solid powder
Density
1.54g/cm3
Boiling Point
397ºC
LogP
5.98
Hydrogen Bond Donor Count
0
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
4
Heavy Atom Count
30
Complexity
792
Defined Atom Stereocenter Count
0
SMILES
C1=CC(=C(C=C1N=C=S)S(=O)(=O)[O-])/C=C/C2=C(C=C(C=C2)N=C=S)S(=O)(=O)[O-].[Na+].[Na+]
InChi Key
GEPAYBXVXXBSKP-SEPHDYHBSA-L
InChi Code
InChI=1S/C16H10N2O6S4.2Na/c19-27(20,21)15-7-13(17-9-25)5-3-11(15)1-2-12-4-6-14(18-10-26)8-16(12)28(22,23)24;;/h1-8H,(H,19,20,21)(H,22,23,24);;/q;2*+1/p-2/b2-1+;;
Chemical Name
disodium;5-isothiocyanato-2-[(E)-2-(4-isothiocyanato-2-sulfonatophenyl)ethenyl]benzenesulfonate
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~250.76 mM)
H2O : ~33.33 mg/mL (~66.86 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.17 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0061 mL 10.0305 mL 20.0610 mL
5 mM 0.4012 mL 2.0061 mL 4.0122 mL
10 mM 0.2006 mL 1.0030 mL 2.0061 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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