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Purity: ≥98%
AS1517499 is a potent STAT6 inhibitor with IC50 of 21 nM. The STAT6 (signal transducers and activators of transcription 6) protein is activated by interleukin (IL)-4 and IL-13, and plays an important role in T-helper cell 2 (Th2) differentiation. STAT6 might therefore be an excellent therapeutic target for various allergic conditions, including asthma and atopic diseases. It shows potent STAT6 inhibition with an IC50 value of 21 nM, and also inhibits IL-4-induced Th2 differentiation of mouse spleen T cells with an IC50 value of 2.3 nM and without influencing T-helper cell 1 (Th1) differentiation induced by IL-12. AS1517499 selectively inhibits Th2 differentiation without affecting Th1 differentiation.
| ln Vitro |
Without influencing IL-12-induced T helper 1 (Th1) cells, AS1517499 demonstrated strong STAT6 inhibition with an IC50 value of 21 nM. It also inhibited IL-4-induced Th2 differentiation of mouse splenic T cells with an IC50 value of 2.3 nM. distinction. Without impacting Th1 differentiation, AS1517499 specifically inhibits Th2 differentiation [1]. Co-incubation inhibits events. IL-13 (100 ng/mL) phosphorylated STAT6 and upregulated RhoA, a monomeric GTPase responsible for smooth muscle contraction's Ca2+ sensitivity in cultured human BSM cells. Both of these effects were linked to AS1517499 (100 nM)[2].
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| ln Vivo |
Following the final ovalbumin antigen challenge, BALB/c mice that had been repeatedly and actively sensitized to the antigen showed elevated IL-13 levels in bronchoalveolar lavage fluid and STAT6 phosphorylation in bronchial tissue. In response to acetylcholine, these mice exhibit increased BSM contractility, and bronchial tissue has higher RhoA expression. A single ovalbumin exposure hour prior to each injection of AS1517499 (10 mg/kg) intraperitoneally virtually eliminated antigen-induced RhoA upregulation and BSM hyperresponsiveness [2].
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| References |
[1]. Nagashima S, et al. Synthesis and evaluation of 2-{[2-(4-hydroxyphenyl)-ethyl]amino}pyrimidine-5-carboxamide derivatives as novel STAT6 inhibitors. Bioorg Med Chem. 2007 Jan 15;15(2):1044-55.
[2]. Chiba Y, et al. A novel STAT6 inhibitor AS1517499 ameliorates antigen-induced bronchial hypercontractility in mice. Am J Respir Cell Mol Biol. 2009 Nov;41(5):516-24 |
| Molecular Formula |
C20H20CLN5O2
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| Molecular Weight |
397.86
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| CAS # |
919486-40-1
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| Related CAS # |
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| SMILES |
O=C(C1=CN=C(NCCC2=CC=C(O)C(Cl)=C2)N=C1NCC3=CC=CC=C3)N
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| Chemical Name |
5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-4-methylbenzamide
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| Synonyms |
AS-1517499; AS1517499; AS 1517499
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 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 (6.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5134 mL | 12.5672 mL | 25.1345 mL | |
| 5 mM | 0.5027 mL | 2.5134 mL | 5.0269 mL | |
| 10 mM | 0.2513 mL | 1.2567 mL | 2.5134 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.
Inhibitory effects of AS1517499 (AS) on the IL-13–induced activation of STAT6 and up-regulation of RhoA in cultured hBSMCs.Am J Respir Cell Mol Biol.2009 Nov;41(5):516-24. |
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Inhibitory effects of AS on the antigen-induced up-regulation of RhoA in bronchial tissues of sensitized mice.Am J Respir Cell Mol Biol.2009 Nov;41(5):516-24. |
Effects of AS1517499 on Serum IgE, IL-13 in BAL Fluids, and Inflammatory Cell Infiltration.Am J Respir Cell Mol Biol.2009 Nov;41(5):516-24. |
Effects of AS on the antigen-induced production of IgE and IL-13 and infiltration of inflammatory cells into the airways in mice.Am J Respir Cell Mol Biol.2009 Nov;41(5):516-24. |
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Antigen-induced activation of signal transducer and activator of transcription 6 (STAT6) in lungs and bronchial tissues of sensitized mice.Am J Respir Cell Mol Biol.2009 Nov;41(5):516-24. |
The effect of compound2ton cytokine production in T cells from spleen of mice.Bioorg Med Chem.2007 Jan 15;15(2):1044-55. |
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