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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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S107 hydrochloride is a novel, potent, and RyR-selective 1,4-benzothiazepine analogue that stabilizes RyR2 channels by increasing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.
Targets |
RyR2/FKBP12.6 complex
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ln Vitro |
S107, a novel RyR2-specific compound, inhibits channel leak, stops cardiac arrhythmias, and raises the threshold for seizures while improving the binding of calstabin2 to the mutant Ryr2-R2474S channel.[1]
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References |
Molecular Formula |
C₁₁H₁₆CLNOS
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Molecular Weight |
245.77
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Exact Mass |
245.0641130
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CAS # |
1357476-46-0
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Related CAS # |
1357476-46-0
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Appearance |
Solid
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SMILES |
CN1CCSC2=C(C1)C=C(C=C2)OC.Cl
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InChi Key |
PKLKSAHANRLKJK-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C11H15NOS.ClH/c1-12-5-6-14-11-4-3-10(13-2)7-9(11)8-12;/h3-4,7H,5-6,8H2,1-2H3;1H
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Chemical Name |
7-methoxy-4-methyl-3,5-dihydro-2H-1,4-benzothiazepine;hydrochloride
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Synonyms |
S107; S-107; S 107
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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) |
Water: ~49 mg/mL (~199.4 mM)
Ethanol: ~10 mg/mL (~40.7 mM) DMSO: ~24 mg/mL (~97.7 mM) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.0688 mL | 20.3442 mL | 40.6884 mL | |
5 mM | 0.8138 mL | 4.0688 mL | 8.1377 mL | |
10 mM | 0.4069 mL | 2.0344 mL | 4.0688 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.
RyR2-homozygous R2474S knock-in mice exhibit increased embryonic lethality that is reduced by a novel RyR2 stabilizing drug (S107) that inhibits Ca2+ leak. J Clin Invest. 2008 Jun 2; 118(6): 2230–2245. td> |
Hippocampal Ryr2RS/WT brain slices and channels exhibit burst activity, which can be inhibited by treatment with ryanodine or the RyR-stabilizing drug S107, respectively. J Clin Invest. 2008 Jun 2; 118(6): 2230–2245. td> |
Fixing the leak in mutant channels from Ryr2RS/WT mice with S107 protects against fatal cardiac arrhythmias. J Clin Invest. 2008 Jun 2; 118(6): 2230–2245. td> |
Electrical and Ca2+ cycling abnormalities in Ryr2RS/WT cardiomyocytes are consistent with Ca2+-triggered afterdepolarizations and are reduced by the RyR2-stabilizing drug S107. J Clin Invest. 2008 Jun 2; 118(6): 2230–2245. td> |
RyR2 channels from heterozygous Ryr2RS/WT hearts show a gain-of-function defect that is rescued by S107 treatment. J Clin Invest. 2008 Jun 2; 118(6): 2230–2245. td> |