| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
ER-27319 maleate targets spleen tyrosine kinase (Syk), a non-receptor tyrosine kinase that plays a critical role in FcεRI-mediated signaling in mast cells. By selectively inhibiting Syk kinase, the compound blocks the tyrosine phosphorylation of Syk and downstream signaling pathways essential for mast cell degranulation and allergic mediator release.
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| ln Vitro |
ER-27319 (maleate) (10-30 μM, 10 min) double inhibits FcεRI γ phosphorylated immunoreceptor tyrosine activation motif-induced SYK tyrosinase with an IC50 value of about 10 μM. Trunk Peptide-induced inositol phosphate production, arachidonic acid release, histamine, and tumor cytokine alpha outcome in RBL-2H3 cells, tumor peritoneum, and human cultured mast cells [1]. In Jurkat cells, ER-27319 (maleate) at 100 μM for 60 minutes does not prevent CD3-stimulated ZAP-70 tyrosine phosphorylation [1]. Maleate (ER-27319) (acid phosphorylation [1], 100 μM, 10 min) anti-IgG increases canine skin tumor-derived mast cells' tyrosine phosphorylation, which inhibits tyrosine phosphorylation (38, 70 kD), and tyrosine antibody Western Blot analysis lowers the other two proteins (62, 80 kD) [1].
ER-27319 maleate is a selective Syk kinase inhibitor that inhibits tyrosine phosphorylation of Syk initiated by FcεRI engagement in rat and human mast cells. The compound inhibits the release of antigen-induced allergic mediators from mast cells through selective inhibition of Fcε receptor I-mediated activation of Syk. |
| ln Vivo |
Specific in vivo efficacy data for ER-27319 maleate are not extensively detailed in standard reference sources. As a Syk inhibitor, it would be expected to show efficacy in animal models of allergic diseases by inhibiting mast cell degranulation and allergic mediator release. Studies in models of asthma, allergic rhinitis, or anaphylaxis would be required to fully characterize its in vivo effects.
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| Enzyme Assay |
ER-27319 maleate's inhibition of Syk kinase activity can be assessed using in vitro kinase assays. Recombinant Syk kinase is incubated with its substrate (e.g., a peptide or protein substrate) and ATP in the presence of varying concentrations of ER-27319 maleate. The amount of phosphorylated substrate is measured using a suitable detection method (e.g., ELISA, Western blot, or radiometric assay) to determine the IC50.
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: Jurkat cells Tested Concentrations: 3, 10, 30, 100 μM Incubation Duration: 10, 30, 60 minutes Experimental Results: No inhibition of tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation. The cellular activity of ER-27319 maleate is evaluated in mast cell models such as rat basophilic leukemia (RBL-2H3) cells or primary human mast cells. Cells are sensitized with IgE and stimulated with antigen in the presence of increasing concentrations of ER-27319 maleate. Mast cell degranulation is measured by β-hexosaminidase or histamine release assays. Syk phosphorylation and downstream signaling are assessed by Western blot. |
| Animal Protocol |
ER-27319 maleate would be administered via intraperitoneal or oral routes in animal models of allergic diseases. In models of passive cutaneous anaphylaxis or ovalbumin-induced asthma, the compound would be given at various doses. Mast cell degranulation, mediator release (histamine, leukotrienes), and inflammatory cell infiltration would be assessed.
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| ADME/Pharmacokinetics |
ER-27319 maleate has a molecular formula of C22H24N2O5 and a molecular weight of 396.44 g/mol. It is an acridone-based compound and the maleate salt of ER-27319. The powder can be stored at -20°C for 3 years, and in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
The toxicity profile of ER-27319 maleate is not extensively documented. As a Syk kinase inhibitor, potential adverse effects may include immunosuppression. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References |
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| Additional Infomation |
ER 27319 maleate is a selective inhibitor of Syk kinase.
ER-27319 maleate (CAS# 1204480-26-1) is a selective Syk kinase inhibitor. It inhibits tyrosine phosphorylation of Syk in mast cells and blocks the release of antigen-induced allergic mediators. The compound has potential utility in the treatment of allergic diseases. |
| Molecular Formula |
C20H22N2O5
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|---|---|
| Molecular Weight |
370.405
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| Exact Mass |
396.168
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| CAS # |
1204480-26-1
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| Related CAS # |
ER-27319;201010-95-9
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| PubChem CID |
56972172
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| Appearance |
Yellow to orange solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
502
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C2=C(C=C1)C(=O)C3=CC=CC=C3N2CCCN)C.C(=C\C(=O)O)\C(=O)O
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| InChi Key |
IIELZHYJYZBSGG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20N2O.C2H2O4/c1-12-8-9-15-17(13(12)2)20(11-5-10-19)16-7-4-3-6-14(16)18(15)213-1(4)2(5)6/h3-4,6-9H,5,10-11,19H2,1-2H3(H,3,4)(H,5,6)
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| Chemical Name |
10-(3-Aminopropyl)-3,4-dimethyl-9-acridone oxalate
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| Synonyms |
ER-27319ER27319
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6997 mL | 13.4986 mL | 26.9971 mL | |
| 5 mM | 0.5399 mL | 2.6997 mL | 5.3994 mL | |
| 10 mM | 0.2700 mL | 1.3499 mL | 2.6997 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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