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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 20 mg/mL, clear
储存温度
2-8°C
SMILES字符串
O=C(NC1=CC=C(C2=C(OC)C=CC(OC)=C2)C=C1)C3=CC=NC=C3F
InChI key
GFEIWXNLDKUWIK-UHFFFAOYSA-N
应用
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)。
一种选择性的 SOCE 抑制剂,可阻止 CRAC 电流(ICRAC),而没有明显的脱靶效价或亲和力。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Jing Li et al.
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
Marjolaine Debant et al.
Journal for immunotherapy of cancer, 7(1), 111-111 (2019-04-25)
Dysregulation in calcium (Ca2+) signaling is a hallmark of chronic lymphocytic leukemia (CLL). While the role of the B cell receptor (BCR) Ca2+ pathway has been associated with disease progression, the importance of the newly described constitutive Ca2+ entry (CE)
Antonio Di Sabatino et al.
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
Siaw Wei Ng et al.
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
Xuexin Zhang et al.
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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