IRAK inhibitor 6 |
Catalog No.GC17371 |
An IRAK4 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1042672-97-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 0.16 μM for IRAK-4
IRAK inhibitor 6 is an interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor.
The interleukin-1 receptor associated kinases (IRAKs) are a family of serine/threonine kinases related with regulating cellular signalling downstream of the IL-18, IL-1 and various Toll-like receptors. IRAK-4 is reported to be essential for the activation of the intracellular signalling cascades including NFКB and MAPK pathways, which are critical for the production of inflammatory cytokines.
In vitro: A quantitative structure–activity relationship (QSAR) study of IRAK inhibitor 6 and its analogs were conducted by using the genetic algorithm and multiple linear regression (GA-MLR) method [1]. In vitro study showed that compared with its unsubstituted phenyl amide analog, the ortho-substitution with chloro, methoxy and difluoromethoxy analogs of IRAK inhibitor 6 improved potency against IRAK-4 significantly. These potency effects were additive, with the most active example in the set being IRAK inhibitor 6, in which the presence of nitrogen-linked substituents at the para position had a beneficial effect on the rate of turnover by human microsomes (20 μL/min/mg protein) [2].
Clinical trial: N/A
References:
[1] Pourbasheer E, Riahi S, Ganjali MR, Norouzi P. Quantitative structure-activity relationship (QSAR) study of interleukin-1 receptor associated kinase 4 (IRAK-4) inhibitor activity by the genetic algorithm and multiple linear regression (GA-MLR) method. J Enzyme Inhib Med Chem. 2010 Dec;25(6):844-53.
[2] Buckley GM, Gowers L, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V, Fraser JL. IRAK-4 inhibitors. Part 1: a series of amides. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3211-4.
Cas No. | 1042672-97-8 | SDF | |
Chemical Name | N-(2-methoxy-4-morpholin-4-ylphenyl)-2-pyridin-3-yl-1,3-thiazole-4-carboxamide | ||
Canonical SMILES | COC1=C(C=CC(=C1)N2CCOCC2)NC(=O)C3=CSC(=N3)C4=CN=CC=C4 | ||
Formula | C20H20N4O3S | M.Wt | 396.46 |
Solubility | ≥ 9.9 mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.5223 mL | 12.6116 mL | 25.2232 mL |
5 mM | 0.5045 mL | 2.5223 mL | 5.0446 mL |
10 mM | 0.2522 mL | 1.2612 mL | 2.5223 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
(Based on Reviews and 30 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *