AF3485 (Synonyms: CAY10686) |
Katalog-Nr.GC18882
One-Click Copy Product Info
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AF3485 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE2 but not PGF2α in A549 cells stimulated with IL-1β (IC50s = 2.9 and >100 µM, respectively).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1195786-61-8
Sample solution is provided at 25 µL, 10mM.
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Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.[1] Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.[2] AF3485 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE2 but not PGF2α in A549 cells stimulated with IL-1β (IC50s = 2.9 and >100 µM, respectively).[3] It reduces inflammatory pain (acetic acid-induced writhing) in mice by 74% when given intraperitoneally at 10 mg/kg.[3] AF3485 is absorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.[3]
References
1. Jakobsson, P.J., Thorén, S., Morgenstern, R., et al. Identification of human prostaglandin E synthase: A microsomal, glutathione-dependent, inducible enzyme, constituting a potential novel drug target. Proc. Natl. Acad. Sci. USA 96(13), 7220-7225 (1999).
2. Stichtenoth, D.O., Thorén, S., Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. J. Immunol. 167, 469-474 (2001).
3. Alisi, M.A., Cazzolla, N., Coletta, I., et al. 3-Aminocarbazole compound, pharmaceutical composition containing it and preparation method therefor. PCT/EP2009/055652, 1-38 (2009).
| Cas No. | 1195786-61-8 | SDF | |
| Überlieferungen | CAY10686 | ||
| Chemical Name | N-[9-(2-hydroxyethyl)-9H-carbazol-3-yl]-2-(trifluoromethyl)-benzamide | ||
| Canonical SMILES | OCCN(C1=C2C=CC=C1)C3=C2C=C(NC(C4=CC=CC=C4C(F)(F)F)=O)C=C3 | ||
| Formula | C22H17F3N2O2 | M.Wt | 398.4 |
| Löslichkeit | DMF: 30 mg/ml,DMF:PBS (pH 7.2); (1:7): 0.1 mg/ml,DMSO: 10 mg/ml,Ethanol: 0.3 mg/ml | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.51 mL | 12.5502 mL | 25.1004 mL |
| 5 mM | 502 μL | 2.51 mL | 5.0201 mL |
| 10 mM | 251 μL | 1.255 mL | 2.51 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)