2. GPCR/G Protein Autophagy Epigenetics PI3K/Akt/mTOR TGF-beta/Smad
  3. Guanylate Cyclase Autophagy AMPK TGF-β Receptor
  4. SGC stimulator 1

sGC stimulator 1 是一种羰基硫化物 (COS)/H2S 供体杂化可溶性鸟苷酸环化酶 (sGC) 刺激剂 (EC50 = 496 nM)。sGC stimulator 1 表现出明显的 H2S 释放特性。sGC stimulator 1 通过提高 和 H2S 水平来减少 TGF-β1 处理的心脏成纤维细胞中的纤维化。sGC stimulator 1 通过激活 sGC 和提高 H2S 水平发挥抗纤维化作用。sGC stimulator 1 可用于心力衰竭 (HF) 的研究。

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SGC stimulator 1

SGC stimulator 1 Chemical Structure

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SGC stimulator 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

sGC stimulator 1 is a carbonyl sulfide (COS)/H2S-donor hybrid soluble guanylyl cyclase (sGC) stimulator (EC50 = 496 nM). sGC stimulator 1 exhibits a well-characterized H2S-releasing property. sGC stimulator 1 reduces fibrosis in TGF-β1-treated cardiac fibroblasts by increasing cGMP and H2S levels. sGC stimulator 1 can exert anti-fibrotic effects by activating sGC and increasing H2S. sGC stimulator 1 can be used for the study of heart failure (HF)[1].

体外研究
(In Vitro)

sGC stimulator 1 (25 μM) 的 H2S 释放效率高达 87%[1]。
sGC stimulator 1 (0-100 μM，48 h) 在适宜浓度范围内对新生大鼠 CFs 细胞表现出良好的细胞相容性，且无明显细胞毒性[1]。
sGC stimulator 1 (0-100 μM，48 h) 在新生大鼠分离的心脏成纤维细胞 (CFs) 中表现出良好的细胞相容性，在适当的浓度范围内无明显的细胞毒性[1]。
sGC stimulator 1 (5-20 μM) 在浓度大于 10 μM 时，可显著提高 CFs 细胞内 cGMP 水平[1]。
sGC stimulator 1 (2.5-10 μM, 48 h) 可有效抑制 TGFβ1 诱导的 CFs 中 α-SMA 表达和 FN 介导的 ECM 合成增加，表明其在抑制 CF 活化方面具有协同作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SGC stimulator 1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: Cardiac fibroblasts isolated from neonatal rats.
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time: 48 h
Result: Indicated good cytocompatibility.
Showed no obvious cytotoxicity within a proper range of concentrations in CFs isolated from neonatal rats.

Western Blot Analysis[1]

Cell Line: Cardiac fibroblasts isolated from neonatal rats.
Concentration: 0 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time: 48 h
Result: Effectively inhibited TGFβ1-induced α-SMA and FN expression in CFs.
体内研究
(In Vivo)

sGC stimulator 1 (3mg/kg、5mg/kg，腹腔注射，每日一次，持续 3 周) 能有效改善异丙肾上腺素 (ISO) (HY-B1670) 诱导的心力衰竭小鼠的心脏收缩和舒张功能，减少心脏扩大和心室重塑，并以剂量依赖性方式增加血浆 H2S 水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Isoproterenol was subcutaneously injected at a dose of 5 mg/kg/day for 3 weeks to Male C57BL/6J mice aged 8 to 10 weeks to establish myocardial fibrosis in mice[1].
Dosage: 3 mg/kg, 5 mg/kg
Administration: Once daily, i.p.
Result: Enhanced EF and FS in a dose-dependent manner, while reducing the enddiastolic and end-systolic volumes as well as end-diastolic and end-systolic inner diameters, indicating a pronounced therapeutic efficacy on cardiac remodeling.
Significantly reduced the ratios of ventricular weight to body weight and ventricular weight to tibia length.
Significantly increased the plasma H2S concentration in a dose-dependent manner, 17.24 μM in the low-dose group (3.0 mg/kg/day) and 39.39 μM in the high-dose group (10 mg/kg/day).
分子量

476.52

Formula

C21H18F2N4O3S2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SGC stimulator 1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SGC stimulator 1SGC stimulator1SGC stimulator-1Guanylate CyclaseAutophagyAMPKTGF-β ReceptorAMP-activated protein kinaseTransforming growth factor beta receptorsHeart FailureHFSoluble Guanylyl CyclasesGCTransforming Growth Factor-Beta 1TGF-β1IsoproterenolISOInhibitorinhibitorinhibit

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