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S107

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Chemical Structure| 927871-76-9 同义名 : -
CAS号 : 927871-76-9
货号 : A248091
分子式 : C11H15NOS
纯度 : 99%+
分子量 : 209.308
MDL号 : MFCD12546447
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(501.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 S107 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. 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. 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[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 to 25%[4]. S107 restored elevated intracellular Ca2+ to normal levels and ameliorated cardiomyocyte contractile properties in isolated cardiomyocytes from 6-month-old Rbm20 KO rats[5]. S107 is able to restore motor function in aging Drosophila to young levels, and this effect of S107 is absent in calstabin (FK506-BP2) mutants[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.78mL

0.96mL

0.48mL

23.89mL

4.78mL

2.39mL

47.78mL

9.56mL

4.78mL
参考文献

[1]Matecki S, Dridi H, et al. Leaky ryanodine receptors contribute to diaphragmatic weakness during mechanical ventilation. Proc Natl Acad Sci U S A. 2016 Aug 9;113(32):9069-74.

[2]Bellinger AM, Reiken S, et al. Hypernitrosylated ryanodine receptor calcium release channels are leaky in dystrophic muscle. Nat Med. 2009 Mar;15(3):325-30.

[3]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

[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

[5]Guo W, Zhu C, Yin Z, Zhang Y, Wang C, Walk AS, Lin YH, McKinsey TA, Woulfe KC, Ren J, Chew HG Jr. The ryanodine receptor stabilizer S107 ameliorates contractility of adult Rbm20 knockout rat cardiomyocytes. Physiol Rep. 2021 Sep;9(17):e15011

[6]Kreko-Pierce T, Azpurua J, Mahoney RE, Eaton BA. Extension of Health Span and Life Span in Drosophila by S107 Requires the calstabin Homologue FK506-BP2. J Biol Chem. 2016 Dec 9;291(50):26045-26055