S107是Type 1 ryanodine receptor (RyR1)稳定剂，可结合RyR1并增强calstabin-1的结合亲和力。 Information S107 is aType 1 ryanodine receptor (RyR1)stabilizer that binds RyR1 and enhances the binding affinity of calstabin-1. In vitro activity S107 is a small compound that enhances calstabin2 binding to RyR2 at low nanomolar concentrations and failed to interact with over 400 receptors, enzymes, and ion channels in screens using up to 10 μM of the compound. S107 has no effect on cardiac ion channels including the voltage-gated Na+, K+, and Ca2+ channels at concentrations up to 10 μM, and S107 had no effect on normal Ca2+ signaling in cells. S107 is a promising candidate drug for treating catecholaminergic polymorphic ventricular tachycardia (CPVT). S107 exerts an antiarrhythmic effect on CPVT-hiPSC-CMs. Pre-incubation with 10 μM S107, which stabilizes the closed state of the ryanodine receptor 2, significantly decreases the percentage of CPVT-hiPSC-CMs presenting DADs to 25%. S107 is thought to improve skeletal muscle function by stabilizing the RyR1-FKBP12 complex. S107 increases FKBP12 binding to RyR1 in SR vesicles in the presence of reduced glutathione and the NO-donor NOC12, with no effect in the presence of oxidized glutathione. S107 can reverse the harmful effects of redox active species on SR Ca2+ release in skeletal muscle by binding to RyR1 low affinity sites. Application It is a labelled benzothiazepine derivative that binds the RyR1 channel and enhances the binding affinity of Calstabin-1. By preventing the depletion of Calstabin-1 from the RyR1 complex, S 107 slows muscle fatique and reduces muscle damage in exercised mice. In a murine model of Duchenne muscular dystrophy, S 107 reduces biochemical and histological evidence of the muscle damage associated with muscular dystrophy, improves muscle function, and increases exercise performance.
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S107
Dangerous GoodsCAS number：927871-76-9 molecular formula：C11H15NOS
overview
compound introduction
Specs
| Chinese alias | 2,3,4,5-四氢-7-甲氧基-4-甲基-1,4-苯并硫氮杂卓 | 7-甲氧基-4-甲基-2,3,4,5-四氢苯并[f][1,4]硫氮杂卓 | ||
| English alias | A12716 | 7-methoxy-4-methyl-3,5-dihydro-2H-1,4-benzothiazepine | EX-A2503 | S-107;S 107 | 7-Methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine | A920274 | AC-35795 | FT-0760478 | 2,3,4,5-Tetrahydro-7-methoxy-4-methyl-1,4-benzothiazepine, analytica | ||
| CAS number | 927871-76-9 | molecular formula | C11H15NOS |
| molecular weight | 209.31 g/mol | Exact mass | ≥98% |
| PSA | 37.800 Ų | logp | 2.000 |
numbering system
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physicochemical properties
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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