| Size | Price | Stock | Qty |
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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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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
S107 is a Type 1 ryanodine receptor (RyR1) stabilizer; binds RyR1 and enhances the binding affinity of calstabin-1. Inhibits Ca leak from the sarcoplasmic reticulum (SR).
| ln Vitro |
At low nanomolar concentrations, S107 is a small molecule that improves calcitonin 2 binding to RyR2. At doses up to 10 μM, it does not interact with over 400 absorbers, enzymes, and ion channels in the screen. Impact S107 affects CPVT-hiPSC-CMs in an antiarrhythmic manner. 10 μM By 25%, S107 pre-stabilizes Ryanodine 2's off-state, thereby lowering the DADs that CPVT-hiPSC-CMs present[2]. When reducing glutathione and the NO donor NOC12 were present, S107 binding enhanced FKBP12 binding to RyR1 in SR vesicles; however, it had no effect when oxidative glutathione was present. Through the RyR1 low-affinity site, S107 can counteract the detrimental effects of redox active drugs on the release of SR Ca2+ in dividing muscles [3].
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| ln Vivo |
S107 can reduce arrhythmias and intermittent feedback, but it does not block the channel or alter the regular Ca2+ signal [1].
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| References |
[1]. Lehnart SE, et al. Leaky Ca2+ release channel/ryanodine receptor 2 causes seizures and sudden cardiac death in mice. J Clin Invest. 2008 Jun;118(6):2230-45.
[2]. Sasaki K, et al. Patient-Specific Human Induced Pluripotent Stem Cell Model Assessed with Electrical Pacing Validates S107 as a Potential Therapeutic Agent for Catecholaminergic Polymorphic Ventricular Tachycardia. PLoS One. 2016 Oct 20;11(10):e0164795. [3]. Mei Y, et al. Stabilization of the skeletal muscle ryanodine receptor ion channel-FKBP12 complex by the 1,4-benzothiazepine derivative S107. PLoS One. 2013;8(1):e54208 |
| Exact Mass |
209.087
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|---|---|
| Elemental Analysis |
C, 63.12; H, 7.22; N, 6.69; O, 7.64; S, 15.32
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| CAS # |
927871-76-9
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| Related CAS # |
1357476-46-0 (HCl);927871-76-9;
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| PubChem CID |
24763624
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| Appearance |
Solid powder
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| LogP |
2.17
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
14
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| Complexity |
188
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
2,3,4,5-Tetrahydro-7-methoxy-4-methyl-1,4-benzothiazepine
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| InChi Code |
BGVCEGVSQDOGSB-UHFFFAOYSA-N
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| Chemical Name |
S107 S-107 S 107.
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| Synonyms |
S107
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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 : ~100 mg/mL (~477.76 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.94 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 (11.94 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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