YM 90709Interleukin-5 receptor antagonist CAS# 163769-88-8 |
- YM155
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| Cas No. | 163769-88-8 | SDF | Download SDF |
| PubChem ID | 1103147 | Appearance | Powder |
| Formula | C22H21N3O2 | M.Wt | 359.43 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 62.5 mg/mL (173.89 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble) | ||
| SMILES | CC1(CC2=CC(=C(C=C2C3=CC4=NC5=CC=CC=C5N=C4N31)OC)OC)C | ||
| Standard InChIKey | HIXSPVQXXDULHS-UHFFFAOYSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Novel, selective inhibitor of interleukin-5 (IL-5) (IC50 = 0.45 - 1 mM). Inhibits IL-5-prolonged eosinophil survival and IL-5-induced tyrosine phosphorylation of JAK2 without inhibiting GM-CSF-mediated effects. Inhibits antigen-induced eosinophil and lymphocyte recruitment in rat airways in vivo, without affecting peripheral blood or bone marrow leukocytes. |
YM 90709 Dilution Calculator
YM 90709 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.7822 mL | 13.9109 mL | 27.8218 mL | 55.6437 mL | 69.5546 mL |
| 5 mM | 0.5564 mL | 2.7822 mL | 5.5644 mL | 11.1287 mL | 13.9109 mL |
| 10 mM | 0.2782 mL | 1.3911 mL | 2.7822 mL | 5.5644 mL | 6.9555 mL |
| 50 mM | 0.0556 mL | 0.2782 mL | 0.5564 mL | 1.1129 mL | 1.3911 mL |
| 100 mM | 0.0278 mL | 0.1391 mL | 0.2782 mL | 0.5564 mL | 0.6955 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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YM-90709 is a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. Target: IL-5 in vitro: YM-90709 potently inhibits the binding of 100 pM [125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells with IC50 values of 1.0±0.40 and 0.57±0.21 μM, respectively. YM-90709 inhibits the 4 pM IL-5-induced effect in a concentration-dependent manner with an IC50 value of 0.45±0.024 μM. YM-90709 also inhibits the higher concentrations (12 and 40 pM) of IL-5-induced effects with IC50 values of 0.89±029 and 1.0±0.22 μM, respectively. [1] YM-90709 is a novel interleukin-5 receptor antagonist, YM-90709 inhibits antigen-induced eosinophil recruitment into the airway, the same as anti-IL-5 mAb does. YM-90709 inhibits the binding of IL-5 to IL-5R on human eosinophils, but did not inhibit the binding of GM-CSF to GM-CSFR. In addition, YM-90709 inhibits IL-5-induced, but not GM-CSF-induced, eosinophil survival as well as the tyrosine phosphorylation of Janus kinase 2. [2] in vivo: YM-90709 suppresses antigen-induced airway inflammation in Brown Norway rats . YM-90709 is a novel IL-5R antagonist with those of anit-IL-5 mAb on the antigen-induced infiltration of eosinophils into the airways of BDF1 mice, a strain that is commonly used in the antibody estimation. [2] This is the first report on the examination of the effects of YM-90709 in vivo, as a novel IL-5R antagonist on the antigen-induced infiltration of eosinophils and other leukocytes into the BALF of Brown-Norway (BN) rats. [3]
References:
[1]. Morokata T, et al. Characterization of YM-90709 as a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. Int Immunopharmacol. 2002 Nov;2(12):1693-702.
[2]. Morokata T, et al. Effect of a novel interleukin-5 receptor antagonist, YM-90709, on antigen-induced eosinophil infiltration into the airway of BDF1 mice. Immunol Lett. 2005 Apr 15;98(1):161-5.
[3]. Morokata T, et al. Effect of a novel interleukin-5 receptor antagonist, YM-90709 (2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline), on antigen-induced airway inflammation in BN rats. Int Immunopharmacol. 2004 Jul;4(7):873-83.
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Effect of a novel interleukin-5 receptor antagonist, YM-90709 (2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline), on antigen-induced airway inflammation in BN rats.[Pubmed:15182727]
Int Immunopharmacol. 2004 Jul;4(7):873-83.
Interleukin-5 (IL-5) plays an important role in the activation of eosinophils in the allergic inflammation in conditions such as asthma, rhinitis, and atopic dermatitis. A newly synthesized compound, YM-90709 (2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline), was previously reported to inhibit the binding of IL-5 to its receptor (R) on human eosinophils and eosinophilic HL-60 clone 15 cells. However, it did not inhibit the binding of granulocyte-macrophage colony-stimulating factor (GM-CSF) to its receptor on the same cells. In this study, the intravenous injection of YM-90709 resulted in the inhibition of antigen-induced infiltration of eosinophils and lymphocytes, but not neutrophils or monocytes, into the bronchoalveolar lavage fluid (BALF) of Brown-Norway (BN) rats, with ED50 values of 0.32 mg/kg and 0.12 mg/kg, respectively. Two glucocorticoids, dexamethasone and prednisolone, inhibited neutrophil, eosinophil, and lymphocyte infiltration into the BALF. However, both significantly reduced the number of peripheral blood leukocytes and bone marrow leukocytes. In contrast, YM-90709 did not affect the peripheral blood leukocytes or the bone marrow leukocytes. These results indicate that, in this model, YM-90709, which is a novel IL-5 R antagonist, inhibits antigen-induced eosinophil and lymphocyte recruitment into the airway, without any suppressive effects on peripheral blood leukocytes or bone marrow leukocytes, in contrast to the glucocorticoids.
Characterization of YM-90709 as a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor.[Pubmed:12469943]
Int Immunopharmacol. 2002 Nov;2(12):1693-702.
Interleukin-5 (IL-5) plays an important role in the activation of eosinophils in allergic inflammation including asthma and atopic dermatitis. A newly synthesized compound, YM-90709, 2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino [2,3-b]quinoxaline, is reported here to 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. 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).
Effect of a novel interleukin-5 receptor antagonist, YM-90709, on antigen-induced eosinophil infiltration into the airway of BDF1 mice.[Pubmed:15790522]
Immunol Lett. 2005 Apr 15;98(1):161-5.
A newly synthesized compound, YM-90709, 2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline, was previously reported to specifically inhibit the binding of interleukin-5 (IL-5) to its receptor (R) on human eosinophils. In this study, the intravenous injection of YM-90709 inhibited antigen-induced infiltration of eosinophils into the bronchoalveolar lavage fluid (BALF) of BDF1 mice, with an ED(50) value of 0.050mg/kg. Anti-murine IL-5 monoclonal antibody (mAb) also inhibited the infiltration of eosinophils with an ED(50) value of 0.035mg/kg. These results indicate that YM-90709, which is a novel IL-5R antagonist, inhibits antigen-induced eosinophil recruitment into the airway, the same as anti-IL-5 mAb does.
