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S107 {[allProObj[0].p_purity_real_show]}

货号：A248091 Ambeed 开学季，买赠积分，赢豪礼

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 化学结构 CAS号：927871-76-9
S107 化学结构
CAS号：927871-76-9
S107 3D分子结构
CAS号：927871-76-9
S107 化学结构 CAS号：927871-76-9
S107 3D分子结构 CAS号：927871-76-9
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S107 纯度/质量文件 产品仅供科研

货号：A248091 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Ca2+ channel-like protein ↓ Calcium Channel ↓ Cav 2.2 ↓ 其他靶点 纯度
CDC25B-IN-2 ✔ Akt {[allProObj[0].p_purity_real_show]}
Clevidipine ✔ {[allProObj[0].p_purity_real_show]}
Verapamil HCl ✔ {[allProObj[0].p_purity_real_show]}
Amlodipine ✔ {[allProObj[0].p_purity_real_show]}
Amlodipine maleate ✔ {[allProObj[0].p_purity_real_show]}
(+)-cis-Diltiazem HCl ✔ {[allProObj[0].p_purity_real_show]}
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

 		{[allProObj[0].p_purity_real_show]}
Tanshinone IIA sulfonate sodium ✔ {[allProObj[0].p_purity_real_show]}
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

 		{[allProObj[0].p_purity_real_show]}
Dronedarone Hydrochloride ✔ {[allProObj[0].p_purity_real_show]}
Nitrendipine +

Calcium channel, IC50: 95 nM

 		{[allProObj[0].p_purity_real_show]}
Efonidipine HCl monoethanolate ✔ {[allProObj[0].p_purity_real_show]}
Cinnarizine ✔ {[allProObj[0].p_purity_real_show]}
SEA0400 ++

NCX, IC50: 33 nM

 		p38 MAPK,ROS,ERK {[allProObj[0].p_purity_real_show]}
Fasudil HCl ✔ Rho,PKA {[allProObj[0].p_purity_real_show]}
ML-9 ✔ MLCK,Akt {[allProObj[0].p_purity_real_show]}
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		{[allProObj[0].p_purity_real_show]}
Lomerizine 2HCl ✔ {[allProObj[0].p_purity_real_show]}
Efonidipine ✔ {[allProObj[0].p_purity_real_show]}
Levamlodipine ✔ {[allProObj[0].p_purity_real_show]}
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		{[allProObj[0].p_purity_real_show]}
Isradipine ✔ {[allProObj[0].p_purity_real_show]}
Lacidipine ✔ {[allProObj[0].p_purity_real_show]}
Lercanidipine ✔ {[allProObj[0].p_purity_real_show]}
Loureirin B ✔ Potassium Channel {[allProObj[0].p_purity_real_show]}
Tetracaine HCl ✔ {[allProObj[0].p_purity_real_show]}
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		{[allProObj[0].p_purity_real_show]}
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		{[allProObj[0].p_purity_real_show]}
Nicardipine ✔ {[allProObj[0].p_purity_real_show]}
Wilforgine ✔ {[allProObj[0].p_purity_real_show]}
Econazole ✔ {[allProObj[0].p_purity_real_show]}
Ginsenoside Rd ✔ NF-κB {[allProObj[0].p_purity_real_show]}
Fendiline HCl ✔ {[allProObj[0].p_purity_real_show]}
Mesaconitine ✔ {[allProObj[0].p_purity_real_show]}
Tetrandrine ✔ {[allProObj[0].p_purity_real_show]}
Nifedipine ✔ {[allProObj[0].p_purity_real_show]}
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		{[allProObj[0].p_purity_real_show]}
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		{[allProObj[0].p_purity_real_show]}
Azelnidipine ✔ {[allProObj[0].p_purity_real_show]}
Levetiracetam ✔ {[allProObj[0].p_purity_real_show]}
Nimodipine ✔ {[allProObj[0].p_purity_real_show]}
Benidipine HCl ✔ {[allProObj[0].p_purity_real_show]}
Pinaverium bromide ✔ {[allProObj[0].p_purity_real_show]}
Pranidipine ✔ {[allProObj[0].p_purity_real_show]}
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

 		{[allProObj[0].p_purity_real_show]}
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		{[allProObj[0].p_purity_real_show]}
Cilnidipine ✔ {[allProObj[0].p_purity_real_show]}
Cinepazide Maleate ✔ {[allProObj[0].p_purity_real_show]}
Terfenadine ✔ {[allProObj[0].p_purity_real_show]}
YM-58483 ✔ {[allProObj[0].p_purity_real_show]}
Ranolazine ✔ {[allProObj[0].p_purity_real_show]}
Praeruptorin A ✔ p38 MAPK,Akt {[allProObj[0].p_purity_real_show]}
Ranolazine 2HCl ✔ {[allProObj[0].p_purity_real_show]}
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

 		{[allProObj[0].p_purity_real_show]}
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

 		{[allProObj[0].p_purity_real_show]}
Levamlodipine besylate ✔ {[allProObj[0].p_purity_real_show]}
Carboxyamidotriazole Orotate ✔ {[allProObj[0].p_purity_real_show]}
IGS-1.76 ✔ {[allProObj[0].p_purity_real_show]}
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

 		++++

Cav 2.2, IC50: 0.001 μM

 		{[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

S107 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].

S107 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

S107 实验方案

计算器
存储液制备 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

S107 技术信息

CAS号927871-76-9
分子式C11H15NOS
分子量 209.308
别名
运输蓝冰
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

Tags: S107 | 927871-76-9 | S 107 | S-107 | Calstabin 2 Modulator | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | S107 纯度/质量文件 | S107 亚型比较 | S107 生物活性 | S107 参考文献 | S107 实验方案 | S107 技术信息

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