| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Sulindac Sulfide (cis-Sulindac sulfide), a major metabolite of sulindac which is is a nonsteroidal anti-inflammatory drug (NSAID), is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity. .
| ln Vitro |
Sulindac sulfide (100 μM) treatment may induce apoptosis in cells, which would lead to a marked decrease in the expression of all proteins and the generation of Aβ. Sulindac sulfide-secreting Aβ42 had an IC50 value of 30.6±2.8 μM. Up to 100 μM, neither Aβ40 nor Aβ42 secretion nor Notch cleavage was impacted by SSone or naproxen. Sulindac sulfide was found to inhibit γ42-secretase activity in a dose-dependent way. SSide has an IC50 value of 20.2±2.6 μM for blocking γ42 secretase activity in vitro. Sulindac sulfide is not an irreversible or pseudo-irreversible inhibitor, as seen by the slope of the rate versus enzyme concentration plotting decreasing with increasing SSide concentration. Moreover, γ-secretase activity was nearly fully restored when the dialyzed solubilized γ-secretase fraction was prepared with sulindac sulfide in comparison to CHAPSO buffer without sulindac sulfide. Based on these observations, it is highly likely that sulindac sulfide functions as a reversible γ-secretase inhibitor and that the γ-secretase complex is its actual molecular target [1].
|
|---|---|
| References | |
| Additional Infomation |
Sulindac sulfide is an aryl sulfide that is a metabolite of sulindac. A non-steroidal anti-inflammatory drug, which also has anticancer activity. It has a role as a non-steroidal anti-inflammatory drug, an apoptosis inducer and an antineoplastic agent. It is an aryl sulfide, an organofluorine compound and a monocarboxylic acid. It is functionally related to a sulindac.
Sulindac Sulfide is the active metabolite of sulindac, a sulfinylindene derivative with anti-inflammatory, analgesic and antipyretic properties. Sulindac is a nonsteroidal anti-inflammatory drug (NSAID) which inhibits cyclooxygenase (COX-1 and-2)-mediated conversion of arachidonic acid to pro-inflammatory prostaglandins. This agent may possess chemopreventive activity against colorectal tumors through a mechanism that involves the induction of apoptosis. The sulfide metabolite is excreted in the bile and reabsorbed from the intestine, thereby helping to maintain constant blood levels and reduce gastrointestinal side effects. (NCI04) |
| Molecular Formula |
C20H17O2FS
|
|---|---|
| Molecular Weight |
340.41118
|
| Exact Mass |
340.093
|
| CAS # |
49627-27-2
|
| Related CAS # |
Sulindac;38194-50-2;(E/Z)-Sulindac sulfide;32004-67-4;Sulindac sulfide-d3;250608-66-3
|
| PubChem CID |
5352624
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
526.3±50.0 °C at 760 mmHg
|
| Melting Point |
189-191ºC
|
| Flash Point |
272.1±30.1 °C
|
| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.653
|
| LogP |
5.74
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
24
|
| Complexity |
546
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(O)CC(C1=C/2C=CC(F)=C1)=C(C)C2=C\C3=CC=C(SC)C=C3
|
| InChi Key |
LFWHFZJPXXOYNR-MFOYZWKCSA-N
|
| InChi Code |
InChI=1S/C20H17FO2S/c1-12-17(9-13-3-6-15(24-2)7-4-13)16-8-5-14(21)10-19(16)18(12)11-20(22)23/h3-10H,11H2,1-2H3,(H,22,23)/b17-9-
|
| Chemical Name |
2-[(3Z)-6-fluoro-2-methyl-3-[(4-methylsulfanylphenyl)methylidene]inden-1-yl]acetic acid
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~146.88 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.34 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 25.0 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: ≥ 2.5 mg/mL (7.34 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 25.0 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 | 2.9376 mL | 14.6882 mL | 29.3763 mL | |
| 5 mM | 0.5875 mL | 2.9376 mL | 5.8753 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9376 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.
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00841204 | COMPLETEDWITH RESULTS | Drug: sulindac Other: placebo Other: laboratory biomarker analysis |
Precancerous Condition | National Cancer Institute (NCI) | 2009-02 | Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
