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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 20 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
O=C(NC1=CC=C(C2=C(OC)C=CC(OC)=C2)C=C1)C3=CC=NC=C3F
應用
Synta66已用作:
- 作为Ca2+释放激活钙 (CRAC)通道抑制剂,研究其对 ORAI 异构体的影响
- 作为ORAI1阻断剂,研究其对Ca2+进入慢性淋巴细胞白血病(CLL) B细胞的影响
- 作为CRAC阻断剂,研究其对釉质细胞中钙库操纵性Ca2+内流(SOCE)的影响
生化/生理作用
Synta66(S66)是一种 CRAC(Ca2+ 释放激活型 Ca2+)通道抑制剂,可通过毒胡萝卜素抑制人血管平滑肌细胞(VSMC)中细胞内钙库的 Ca2+ 耗尽,从而高效地阻断 SOCE(钙库操纵性钙内流)(IC50 = 26nM & 43 nM,分别基于最大 Ca2+ 水平 & 增加率)。Synta66 对一系列受体和离子通道(例如 L 型 Ca2 + 通道)没有亲和力,并且不影响 TRPC1/5 介导的 SOCE 或钙库操纵性非选择性阳离子电流。据报道,白细胞对 Synta66 对 CRAC 的抑制作用较不敏感(IC50 = 1.76 μM/HL-60、1 µM/Jurkat,1.4 μM/大鼠 RBL)。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Journal of immunology (Baltimore, Md. : 1950), 183(5), 3454-3462 (2009-08-04)
Prolonged Ca(2+) entry through Ca(2+) release-activated Ca(2+) (CRAC) channels is crucial in activating the Ca(2+)-sensitive transcription factor NFAT, which is responsible for directing T cell proliferation and cytokine gene expression. To establish whether targeting CRAC might counteract intestinal inflammation, we
The Journal of biological chemistry, 283(46), 31348-31355 (2008-09-23)
Mast cell activation involves cross-linking of IgE receptors followed by phosphorylation of the non-receptor tyrosine kinase Syk. This results in activation of the plasma membrane-bound enzyme phospholipase Cgamma1, which hydrolyzes the minor membrane phospholipid phosphatidylinositol 4,5-bisphosphate to generate diacylglycerol and
British journal of pharmacology, 164(2), 382-393 (2011-05-07)
The aim was to advance the understanding of Orai proteins and identify a specific inhibitor of the associated calcium entry mechanism in vascular smooth muscle cells (VSMCs). Proliferating VSMCs were cultured from human saphenous veins. Intracellular calcium was measured using
Cell calcium, 91, 102281-102281 (2020-09-09)
The ubiquitous Ca2+ release-activated Ca2+ (CRAC) channel is crucial to many physiological functions. Both gain and loss of CRAC function is linked to disease. While ORAI1 is a crucial subunit of CRAC channels, recent evidence suggests that ORAI2 and ORAI3
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