| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| Targets |
STAT6 0.70 nM (IC50)
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| ln Vitro |
YM-341619 (0.1-100 nM; pretreatment 30 min before IL-4) suppresses IL-4-increased STAT6 luciferase gene activity in a concentration-dependent manner with an IC50 value of 1.5 nM in FW4 cells[2]. In T cells grown with IL-4, YM-341619 (0.1–10 nM; pretreatment 30 min before IL–4) concentration-dependently reduces IL–4 production and GATA-3 mRNA expression. Furthermore, it has no effect on T cells grown with IL-12 on the expression of T-bet (a Th1 transcription factor) mRNA or the generation of IFN-γ[2].
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| ln Vivo |
The CLtot, t1/2, and Vd values of YM-341619 (intravenous injection; 1 mg/kg) are 36.1 mL/min/kg, 1.0 hour, and 3117 mL/kg, respectively. Additionally, in 8-week-old female balb/c mice, it displays Cmax, Tmax, AUC, and F% values of 80 ng/mL, 0.5h, 114 ng h/mL, and 25%, respectively[1]. The IgE level is dose-dependently suppressed by YM-341619 (oral administration; 0.003-0.03 mg/kg), but not the IgG2a level. YM-341619's ED50 value for the inhibition of IgE production is 0.026 mg/kg. In DNP-sensitized rats, YM-341619 tends to reduce IL-4 and IL-13 production in a dose-dependent way (both 57%), while it has no effect on IFN-γ production[2].
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| Cell Assay |
RT-PCR[2]
Cell Types: T cells Tested Concentrations: 0.1 nM, 1 nM, 10 nM Incubation Duration:Pretreatment 30 min before IL-4, then IL-4 treated for 16 hrs (hours) Experimental Results: diminished IL-4 and GATA-3 mRNA expression. |
| Animal Protocol |
Animal/Disease Models: DNP-Ascaris-sensitized rats[1]
Doses: 0.003- 0.03 mg/kg Route of Administration: Oral administration; 0.003-0.03 mg/kg Experimental Results: Suppressed IL-4 and IL-13 production in splenocytes derived from DNP-ascaris-sensitized rats without reducing IFN-γ production. |
| References |
[1]. Shinya Nagashima, et al. Identification of 4-benzylamino-2-[(4-morpholin-4-ylphenyl)amino]pyrimidine-5-carboxamide derivatives as potent and orally bioavailable STAT6 inhibitors. Bioorg Med Chem. 2008 Jul 1;16(13):6509-21. 9.15
[2]. Keiko Ohga,et al.YM-341619 suppresses the differentiation of spleen T cells into Th2 cells in vitro, eosinophilia, and airway hyperresponsiveness in rat allergic models. Eur J Pharmacol. 2008 Aug 20;590(1-3):409-16. |
| Molecular Formula |
C22H21F3N6O2
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|---|---|
| Molecular Weight |
458.44
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| CAS # |
643082-52-4
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| SMILES |
N(C1=NC(NC2C=CC(N3CCOCC3)=CC=2)=NC=C1C(=O)N)CC1C(=CC=C(F)C=1F)F
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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: 50 mg/mL (109.07 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.45 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 25.0 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: ≥ 2.5 mg/mL (5.45 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 25.0 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: ≥ 2.5 mg/mL (5.45 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 | 2.1813 mL | 10.9066 mL | 21.8131 mL | |
| 5 mM | 0.4363 mL | 2.1813 mL | 4.3626 mL | |
| 10 mM | 0.2181 mL | 1.0907 mL | 2.1813 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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