Synta66是钙离子通道Orai(CRAC的核心)的抑制剂，主要用于神经疾病的研究。
Synta66 is an inhibitor of store-operated calcium entry channel Orai, which forms the pore of the CRAC channel, and used for the research of neurological disease.
Synta66 is an inhibitor of Orai, which forms the pore of the CRAC channel. Synta66 (10 μM) attenuates peak SOCE in Müller glia. Synta66 (10 μM) prevents orai channels mediating the residual SOC current in Trpc1-/- Müller cells[1]. Synta66 (10 μM) nearly completely blocks the Ca2+ entry signal evoked by CaCl2 addition, whereas it moderately reduces Ca2+ mobilization from stores with 10% to 30% in platelet. Synta66 (10 μM) suppresses human platelet activation in plasma and whole-blood thrombus formation. Synta66 (10 μM) also inhibits murine platelet responses and thrombus formation[2]. Synta66 (10 μM) inhibits LAD2 human mast cell line. Synta66 (10 μM) significantly inhibits FcεRI stimulated histamine and TNFα secretion, and has differential effects on FcεRI stimulated prostaglandin D2 and cytokine release in human lung mast cells (HLMCs)[3].
[1]. Molnár T, et al. Store-Operated Calcium Entry in Müller Glia Is Controlled by Synergistic Activation of TRPC and Orai Channels. J Neurosci. 2016 Mar 16;36(11):3184-98. [2]. van Kruchten R, et al. Antithrombotic potential of blockers of store-operated calcium channels in platelets. Arterioscler Thromb Vasc Biol. 2012 Jul;32(7):1717-23. [3]. Wajdner HE, et al. Orai and TRPC channel characterization in FcεRI-mediated calcium signaling and mediator secretion in human mast cells. Physiol Rep. 2017 Mar;5(5).
Cell experiment: | Human Lung Mast Cell (HLMCs) are cultured in DMEM+Glutamax media containing 1% antibiotic-antimycotic solution, 1% non-essential amino acids, 10% fetal calf serum and supplemented with 100 ng/mL human stem cell factor, 50 ng/mL IL-6 and 10 ng/mL IL-10. For histamine assays mast cells are isolated from human lung tissue and used within 24 h[3]. |
参考文献: [1]. Molnár T, et al. Store-Operated Calcium Entry in Müller Glia Is Controlled by Synergistic Activation of TRPC and Orai Channels. J Neurosci. 2016 Mar 16;36(11):3184-98. | |
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