所有图片(1)
别名:
4-吡啶甲酰胺, N-(2′,5′-二甲氧基[1,1′-联苯] -4-基）-3-氟-, GSK1349571A, N-(2′,5′-二甲氧基[1,1′-联苯]-4-yl)-3-氟-4-吡啶甲酰胺, S66, Synta 66, Synta-66
经验公式（希尔记法）:
C20H17FN2O3
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
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
应用
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）。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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
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)
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
Guilherme H Souza Bomfim et al.
Cell calcium, 87, 102187-102187 (2020-03-09)
Calcium (Ca2+) release-activated Ca2+ (CRAC) channels mediated by STIM1/2 and ORAI (ORAI1-3) proteins form the dominant store-operated Ca2+ entry (SOCE) pathway in a wide variety of cells. Among these, the enamel-forming cells known as ameloblasts rely on CRAC channel function
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