|7-甲氧基-4-甲基-2,3,4,5-四氢苯并[f][1,4]硫氮杂盐酸盐|CsnPharm

CAS No.: 1357476-46-0

7-Methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine hydrochloride Catalog No. CSN21356

Synonyms: S107 HCl

S107 HCl is a RyR-selective 1,4-benzothiazepine derivative that stabilizes RyR2 channels by enhancing the binding affinity of calstabin2 to mutant and/or PKA-phosphorylated channels.

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技术信息

生物活性

描述S107 HCl 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). S107 increased 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. Addition of 0.15 µM FKBP12 to SR vesicles prevented FKBP12 dissociation; however, in the presence of oxidized glutathione and NOC12, FKBP12 dissociation was observed in skeletal muscle homogenates that contained 0.43 µM myoplasmic FKBP12 and was attenuated by S107. In single channel measurements with FKBP12-depleted RyR1s, in the absence and presence of NOC12, S107 augmented the FKBP12-mediated decrease in channel activity. S107 can reverse the harmful effects of redox active species on SR Ca(2+) release in skeletal muscle by binding to RyR1 low affinity sites^[2]. Direct rescue of dysfunctional RyR2 (type 2 ryanodine receptor) with dantrolene or rycal S107 reduced diastolic SR (sarcoplasmic reticulum) Ca2+ leak in LA (left atrium) myocytes and prevented atrial burst pacing stimulated AF(atrial fibrillation)^[3]. Pre-incubation with 10 μM S107, which stabilizes the closed state of the ryanodine receptor 2, significantly decreased the percentage of CPVT(catecholaminergic polymorphic ventricular tachycardia)-hiPSC-CMs(cardiomyocytes) presenting DADs (delayed afterdepolarizations) to 25%. The development of DADs in the presence of isoproterenol was significantly suppressed by S107^[4].
参考文献

[2] Mei Y, Xu L, Kramer HF, Tomberlin GH, Townsend C, Meissner G. Stabilization of the skeletal muscle ryanodine receptor ion channel-FKBP12 complex by the 1,4-benzothiazepine derivative S107. PLoS One. 2013;8(1):e54208
[3] Zhang Y, Qi Y, Li JJ, He WJ, Gao XH, Zhang Y, Sun X, Tong J, Zhang J, Deng XL, Du XJ, Xie W. Stretch-induced sarcoplasmic reticulum calcium leak is causatively associated with atrial fibrillation in pressure-overloaded hearts. Cardiovasc Res. 2020 Jun 12:cvaa163
[4] Sasaki K, Makiyama T, Yoshida Y, Wuriyanghai Y, Kamakura T, Nishiuchi S, Hayano M, Harita T, Yamamoto Y, Kohjitani H, Hirose S, Chen J, Kawamura M, Ohno S, Itoh H, Takeuchi A, Matsuoka S, Miura M, Sumitomo N, Horie M, Yamanaka S, Kimura T. 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

1357476-46-0

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H16ClNOS

运输

蓝冰

分子量

245.77

别名

S107 HCl

溶解度

DMSO	insoluble
Water	110.0 mg/mL (447.6 mM)

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7-Methoxy-4-methyl-2,3,4,5-tetrahydrobenzo[f][1,4]thiazepine hydrochloride Catalog No. CSN21356

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