Synta-66

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 CRAC 通道 Orai1 阻断剂，IC50 为 3 uM。

A potent, selective CRAC channel Orai1 blocker with IC50 of 3 uM; does not impair other plasma membrane ion transporters; inhibits antigen-evoked Ca2+ influx in Fura-2-loaded cells at 10 uM, prevents the increase in Syk activity triggered by Ca2+ entry; reduces FcεRI-dependent Ca(2+) influx and the release of histamine, leukotriene C4, and cytokines (IL-5/-8/-13 and TNFα) by up to 50% at 3 uM in HLMCs.

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. 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. 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).

——

Synta 66 | Synta 66 | S66 | GSK1349571A

GPCR/G Protein

Calcium Channel

Calcium Channel

——

——

835904-51-3

352.37

C20H17FN2O3

>98% (HPLC)

DMSO : 77.5 mg/mL 219.95 mM; H2O : < 0.1 mg/mL

COC1=CC(=C(C=C1)OC)C2=CC=C(C=C2)NC(=O)C3=C(C=NC=C3)F

N-(2',5'-Dimethoxy[1,1'-biphenyl]-4-yl)-3-fluoro-4-pyridinecarboxamide

(-20℃)

With Ice Pack

≥ 2 years