| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| Other Sizes |
|
ER 27319 (ER27319; ER-27319), an acridone derivative, is a novel, potent and selective Syk kinase inhibitor with the potential to be used in the treatment of allergic disease. It inhibits the release of antigen-induced allergic mediators from mast cells by selectively inhibiting fcepsilon receptor I-mediated activation of Syk.
| ln Vitro |
In RBL-2H3 cells, tumor peritoneum, and human cultured mast cells, ER-27319 (24 h) decreases the formation of inositol phosphate, the release of arachidonic acid, histamine, and tumor cytokine alpha. Around 10 μM is the approximate value at which the ER-27319 (10-30 μM, 10 min) loop suppresses the tyrosine phosphorylation of SYK caused by the immunoreceptor tyrosine activation motif of FcεRI γ [1]. The tyrosine phosphorylation of ZAP-70 in Jurkat cells caused by CD3 stimulation is not inhibited by ER-27319 (up to 100 μM, 60 min) [1]. Anti-IgG-stimulated canine skin tumor-derived mast cells exhibit decreased tyrosine phosphorylation of two proteins (62, 80 kD) and inhibition of two other proteins (38, 70 kD) upon exposure to ER-27319 (100 μM, 10 min).
|
|---|---|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: RBL-2H3 Cell Tested Concentrations: 10, 30 and 100 μM Incubation Duration: 10 minutes Experimental Results: Inhibition of tyrosine phosphorylation of SYK in mast cells (57% inhibition at 10 and 30 μM, respectively and 87%). Inhibits SYK tyrosine phosphorylation induced by the phospho-γ ITAM of FcεRI γ but not the phospho-Ig β immunoreceptor tyrosine activation motif at 10 and 30 μM . 100 μM has no effect on SYK phosphorylation induced by the Igβ immunoreceptor tyrosine activation motif. Western Blot Analysis[1] Cell Types: Jurkat cells Tested Concentrations: 3, 10, 30, 100 μM Incubation Duration: 10, 30, 60 minutes Experimental Results: ID does not inhibit tyrosine phosphorylation of ZAP-70 in response to anti-CD3 stimulation. |
| References |
|
| Molecular Formula |
C20H22N2O5
|
|---|---|
| Molecular Weight |
396.43636
|
| Exact Mass |
396.169
|
| CAS # |
201010-95-9
|
| Related CAS # |
ER-27319 maleate;1204480-26-1
|
| PubChem CID |
9799508
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.149g/cm3
|
| Boiling Point |
475.894ºC at 760 mmHg
|
| Flash Point |
241.613ºC
|
| Vapour Pressure |
0mmHg at 25°C
|
| Index of Refraction |
1.611
|
| LogP |
3.532
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
27
|
| Complexity |
455
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
IIELZHYJYZBSGG-UHFFFAOYSA-N
|
| 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)21;3-1(4)2(5)6/h3-4,6-9H,5,10-11,19H2,1-2H3;(H,3,4)(H,5,6)
|
| Chemical Name |
10-(3-aminopropyl)-3,4-dimethylacridin-9-one;oxalic acid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.5224 mL | 12.6122 mL | 25.2245 mL | |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL | |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
