Synta66 [835904-51-3]

Cat# HY-111325-1mL

Size : 10mM/1mL

Brand : MedChemExpress

Contact local distributor :


Phone : +1 850 650 7790

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.

IC50 & Target

Orai[1]

Cellular Effect
Cell Line Type Value Description References
Jurkat IC50
10 nM
Compound: 2, Synta
Inhibition of Orai channel in phytohemagglutinin-stimulated human Jurkat E6-1 cells assessed as NFAT-induced transcription measured as IL-2 level after 20 hrs by ELISA
Inhibition of Orai channel in phytohemagglutinin-stimulated human Jurkat E6-1 cells assessed as NFAT-induced transcription measured as IL-2 level after 20 hrs by ELISA
[PMID: 25690784]
Jurkat IC50
82 nM
Compound: 2, Synta
Inhibition of Orai-mediated calcium entry in human Jurkat E6-1 cells after 1 hr by FLIPR assay
Inhibition of Orai-mediated calcium entry in human Jurkat E6-1 cells after 1 hr by FLIPR assay
[PMID: 25690784]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility
In Vitro: 

DMSO : 77.5 mg/mL (219.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.58 mg/mL (7.32 mM); Suspended solution; Need ultrasonic and warming

    This protocol yields a suspended solution of 2.58 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.58 mg/mL (7.32 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 2.58 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

You might also be interested by the following products:



Cat#
Description
Cond.
Price Bef. VAT
102-22435
 400uL 
HY-12521-1mL
 10mM/1mL 
HY-100831-1mL
 10mM/1mL