MedChemExpress -Model Synta66 -835904-51-3

FromMedChemExpress LLC (MCE)

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

MCE China：Synta66

Brand：MedChemExpress (MCE)

Cat. No.HY-111325

CAS：835904-51-3

Purity：98.32%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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].

Cell Assay：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].

IC50 & Target：Orai[1] Cellular Effect Cell Line Type Value Description References

References：

[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. [Content Brief]

[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. [Content Brief]

[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). [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。