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Purity: ≥98%
YM-90709 is a novel antagonist of interleukin-5 receptor which inhibits the binding of interleukin-5 to interleukin-5 receptor. YM-90709 inhibit the binding of IL-5 to its receptor on peripheral human eosinophils and butyric acid-treated eosinophilic HL-60 clone 15 cells, with IC50 values of 1.0 and 0.57 microM, respectively. Interleukin-5 (IL-5) plays an important role in the activation of eosinophils in allergic inflammation including asthma and atopic dermatitis. In contrast, YM-90709 did not affect the binding of granulocyte-macrophage colony-stimulating factor (GM-CSF) to its receptor on eosinophils and eosinophilic HL-60 clone 15 cells. In functional assays, YM-90709 inhibited IL-5-prolonged eosinophil survival with an IC50 value of 0.45 microM and did not affect the GM-CSF-prolonged eosinophil survival. Furthermore, YM-90709 inhibited the IL-5-induced but not GM-CSF-induced tyrosine phosphorylation of Janus kinase 2 (JAK2) in eosinophilic HL-60 clone 15 cells. These results indicate that YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).
| ln Vitro |
YM-90709 (0-100 μM; 1 hour) inhibits [125I]-IL-5 binding to IL-5R on eosinophilic HL-60 clone 15 cells and human peripheral eosinophils[1]. Eosinophilic HL-60 clone 15 cells treated with YM-90709 (0-100 μM; 96 hours) affects IL-5 and GM-CSF and prolongs eosinophil survival[1]. YM-90709 (0-100 μM; 5 min; Eosinophilic HL-60 clone 15 cells) inhibits Janus kinase 2 tyrosine phosphorylation and eosinophil survival induced by IL-5, but not by GM-CSF[2].
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| ln Vivo |
The antigen-induced infiltration of eosinophils and lymphocytes, but not neutrophils or monocytes, into the bronchoalveolar lavage fluid (BALF) of inbred female Brown-Norway (BN) rats is inhibited by YM-90709 (0.01–10 mg/kg; intravenous injection, 72 hours)[2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Purified eosinophils were suspended at 5×105 cells/ml in RPMI-1640 medium. Tested Concentrations: 0.01, 0.1, 1, 10 and 100 μM Incubation Duration: 96 hrs (hours) Experimental Results: The survival time of eosinophils was prolonged. Western Blot Analysis[1] Cell Types: Eosinophilic HL-60 clone 15 cells in RPMI-1640 medium containing 10% FBS, antibiotics, 50 mM 2-ME and 25 mM HEPPES. Tested Concentrations: Incubation Duration: 5 min Experimental Results: decreased the IL-5-induced phosphorylation of JAK2 to near basal levels. |
| Animal Protocol |
Animal/Disease Models: Inbred female Brown-Norway (BN) rats and used at 4-6 weeks of age[2].
Doses: 0.01, 0.1, 1, 10 mg/kg Route of Administration: intravenous (iv) injection; 72 hrs (hours) Experimental Results: Inhibited WBC and eosinophil infiltration in a dose-dependent manner. |
| References |
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| Additional Infomation |
LSM-2128 is a quinoxaline derivative.
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| Molecular Formula |
C22H21N3O2
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|---|---|---|
| Molecular Weight |
359.42
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| Exact Mass |
359.163
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| CAS # |
163769-88-8
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| Related CAS # |
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| PubChem CID |
1103147
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| Appearance |
Brown to orange solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
579.6±50.0 °C at 760 mmHg
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| Flash Point |
304.3±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.666
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| LogP |
5.89
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
556
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HIXSPVQXXDULHS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21N3O2/c1-22(2)12-13-9-19(26-3)20(27-4)10-14(13)18-11-17-21(25(18)22)24-16-8-6-5-7-15(16)23-17/h5-11H,12H2,1-4H3
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| Chemical Name |
16,17-dimethoxy-21,21-dimethyl-1,3,10-triazapentacyclo[11.8.0.02,11.04,9.014,19]henicosa-2,4,6,8,10,12,14,16,18-nonaene
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| Synonyms |
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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 |
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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: ≥ 2.08 mg/mL (5.79 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 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 (5.79 mM) 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; with ultrasonication. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7823 mL | 13.9113 mL | 27.8226 mL | |
| 5 mM | 0.5565 mL | 2.7823 mL | 5.5645 mL | |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7823 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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