| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
CRAC channel 402 nM (IC50) Orai1/Stim1 channels 25 nM (IC50) IL-2
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|---|---|
| ln Vitro |
RO2959 has an IC50 of 25 nM for Orai1 and 530 nM for Orai3 inhibition. With an IC50 value of 265 nM, RO2959 inhibits store operated calcium entry (SOCE) in activated CD4+T lymphocytes[1]. Strong SOCE inhibitor RO2959 inhibits both IP3-dependent current in CRAC-expressing RBL-2H3 cells and CHO cells that exhibit stable human Orai1 and Stim1 expression, as well as SOCE in human primary CD4+ T cells stimulated by TCR activation or thapsigargin therapy. When TCR stimulation or mixed lymphocyte reaction (MLR) is used to stimulate T cells, RO2959 totally blocks both cytokine generation and T cell proliferation[1].
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| References |
[1]. Gang Chen, et al. Characterization of a Novel CRAC Inhibitor That Potently Blocks Human T Cell Activation and Effector Functions. Mol Immunol. 2013 Jul;54(3-4):355-67.
[2]. Changbo Zheng, et al. Gastrodin Inhibits Store-Operated Ca 2+ Entry and Alleviates Cardiac Hypertrophy. Front Pharmacol. 2017 Apr 25;8:222. |
| Molecular Formula |
C21H20CLF2N5OS
|
|---|---|
| Molecular Weight |
463.93
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| CAS # |
2309172-44-7
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| Related CAS # |
RO2959 hydrochloride;1219927-22-6
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
Cl.S1C(C)=CN=C1N1CC(C2C=NC(=CN=2)NC(C2C(=CC=CC=2F)F)=O)=C(C)CC1
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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: 25 mg/mL (53.89 mM)
H2O: < 0.1 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.48 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 sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.48 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), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: ≥ 2.08 mg/mL (4.48 mM) (saturation unknown) 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 | 2.1555 mL | 10.7775 mL | 21.5550 mL | |
| 5 mM | 0.4311 mL | 2.1555 mL | 4.3110 mL | |
| 10 mM | 0.2155 mL | 1.0777 mL | 2.1555 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.
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