| Size | Price | Stock | Qty |
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| 2mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
Synta66 is a novel and potent inhibitor/blocker of Ca2+ entry via store-operated Ca2+ release-activated Ca2+ (CRAC) channels. As an inhibitor of store-operated calcium entry channel Orai, it forms the pore of the CRAC channel, and is used for the research of neurological disease.
| ln Vitro |
The CRAC channel pore is formed by Orai, which is inhibited by Synta66. In Müller glia, Synta66 (10 μM) reduces peak SOCE. In Trpc1−/− Müller cells, synta66 (10 μM) blocks orai channels from mediating residual SOC currents [1]. The Ca2+ entry signal caused by the injection of CaCl2 is nearly entirely blocked by Synta66 (10 μM), whereas the mobilization of stored Ca2+ in platelets is only slightly decreased by 10% to 30%. Human platelet activation in plasma and whole blood thrombosis is inhibited by Synta66 (10 μM). In mice, Synta66 (10 μM) also prevents thrombosis and the platelet response [2]. Synta66 (10 μM) suppresses human mast cell lines' expression of LAD2. Synta66 (10 μM) has varied effects on FcεRI-stimulated prostaglandin D2 and cytokine release in human lung mast cells (HLMC) and strongly suppresses FcεRI-stimulated histamine and TNFα production [3].
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| 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.
[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) |
| Molecular Formula |
C20H17N2O3F
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|---|---|
| Molecular Weight |
352.359
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| CAS # |
835904-51-3
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| SMILES |
O=C(C1=C(F)C=NC=C1)NC2=CC=C(C3=CC(OC)=CC=C3OC)C=C2
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~77.5 mg/mL (~219.95 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.58 mg/mL (7.32 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.58 mg/mL (7.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.58 mg/mL (7.32 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8380 mL | 14.1900 mL | 28.3801 mL | |
| 5 mM | 0.5676 mL | 2.8380 mL | 5.6760 mL | |
| 10 mM | 0.2838 mL | 1.4190 mL | 2.8380 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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