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SN-6 (SN6) is a novel and selective Na+/Ca2+ exchanger (NCX) inhibitor, inhibiting 45Ca2+ uptake by NCX1, NCX2, and NCX3, with IC50s of 2.9, 16, and 8.6 μM, respectively. Also abolishes acetylcholine (ACh)-induced vasodilation.
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| ln Vitro |
Moreover, SN 6 has a higher IC50 of 18 μM and less potently inhibits the muscarinic cholinergic receptor (up to 30 μM). The initial rate of Na+i-dependent 45Ca2+ uptake into Na+-loaded sarcolemmal vesicles is totally inhibited by SN 6 (0.3-30 μM) in a dose-dependent manner (IC50, 5.3 ± 0.37 μM). In parental LLC-PK1 cells and NCX1 transfectants, SN 6 (0.3-10 μM) dose-dependently protects against the hypoxia/reoxygenation-induced LDH release, but not in K229Q transfectants[1]. With IC50 values of 2.3 μM and 1.9 μM, respectively, SN 6 (1-30 μM) inhibits the bidirectional outward and inward INCX in a concentration-dependent manner. Additionally, SN 6 inhibits bidirectional current (INCX) in a way depending on the concentration of [Na+]i; at 10 mM, 20 mM, and 30 mM [Na+]i, respectively, SN 6's IC50 values are 3.4 μM, 2.3 μM, and 1.1 μM[2]. In NCX1 transfectants, SN 6 suppresses hypoxia/reoxygenation-induced LDH release with an IC50 value of 0.63 ± 0.15 μM[3].
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| Cell Assay |
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| References |
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| Molecular Formula |
C20H22N2O5S
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|---|---|
| Molecular Weight |
402.47
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| Exact Mass |
402.125
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| CAS # |
415697-08-4
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| PubChem CID |
10222761
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| Appearance |
White to light yellow solid powder
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| Density |
1.285g/cm3
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| Boiling Point |
581.2ºC at 760mmHg
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| Flash Point |
305.3ºC
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| Index of Refraction |
1.605
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| LogP |
4.162
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
28
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZVYIJXLMBWCGHP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22N2O5S/c1-2-26-20(23)18-13-28-19(21-18)11-14-5-9-17(10-6-14)27-12-15-3-7-16(8-4-15)22(24)25/h3-10,18-19,21H,2,11-13H2,1H3
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| Chemical Name |
ethyl 2-[[4-[(4-nitrophenyl)methoxy]phenyl]methyl]-1,3-thiazolidine-4-carboxylate
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| Synonyms |
SN6 SN 6 SN-6
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~155.29 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.17 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
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 (5.17 mM) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4847 mL | 12.4233 mL | 24.8466 mL | |
| 5 mM | 0.4969 mL | 2.4847 mL | 4.9693 mL | |
| 10 mM | 0.2485 mL | 1.2423 mL | 2.4847 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.
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