AT791 |
Katalog-Nr.GC62334
One-Click Copy Product Info
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AT791 ist ein potenter und oral bioverfÜgbarer TLR7- und TLR9-Inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1219962-49-8
Sample solution is provided at 25 µL, 10mM.
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AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor. AT791 inhibits TLR7 and 9 signaling in a variety of human and mouse cell types and inhibits DNA-TLR9 interaction in vitro[1].
AT791 potently suppresses DNA stimulation of HEK:TLR9 cells, with IC50 of 0.04 μM and is significantly less effective at suppressing R848 stimulation of HEK:TLR7 cells (IC50= 3.33 μM) [1].AT7916 suppresses TLR9-DNA interaction in vitro, with an IC50 in the 1 to10 μM range[1].AT791 and E6446 are typical of "lysosomotropic"compounds in that they are lipophilic and contain weak base amines. At neutral pH, such compounds are nonpolar and can penetrate lipid membranes, but within low pH vesicles they become protonated and are trapped (de Duve et al., 1974). Capillary electrophoresis showed that AT791 has pKas of 7.9 and 6.1, and E6446 has pKas of 8.6 and 6.5, indicating they would be more highly protonated in endolysosomal compartments compared with cytoplasm[1].
Short-term induction of serum interleukin-6 in mice by CpG1668 DNA is effectively suppresses by pretreatment with AT791 (20 mg/kg; p.o.)[1].
[1]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014;85(3):429-440.
| Cas No. | 1219962-49-8 | SDF | |
| Formula | C23H31N3O3 | M.Wt | 397.51 |
| Löslichkeit | DMSO : 25 mg/mL (62.89 mM; Need ultrasonic) | 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. |
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| 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 | 2.5157 mL | 12.5783 mL | 25.1566 mL |
| 5 mM | 503.1 μL | 2.5157 mL | 5.0313 mL |
| 10 mM | 251.6 μL | 1.2578 mL | 2.5157 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)